XIAP

Baculoviral iap repeat-containing protein 4 (x-linked inhibitor of apoptosis protein)

Reviewed UniProt entries for XIAP and its protein partners


UniProt code UniProt Name Protein Name Gene Name Organism Length
Q60989 XIAP_MOUSE Baculoviral IAP repeat-containing protein 4 (EC 6.3.2.-) (E3 ubiquitin-protein ligase XIAP) (IAP homolog A) (Inhibitor of apoptosis protein 3) (IAP-3) (mIAP-3) (mIAP3) (X-linked inhibitor of apoptosis protein) (X-linked IAP) Xiap Aipa Api3 Birc4 Miha Mus musculus (Mouse) 496
Q9R0I6 XIAP_RAT Baculoviral IAP repeat-containing protein 4 (EC 6.3.2.-) (E3 ubiquitin-protein ligase XIAP) (IAP homolog A) (Inhibitor of apoptosis protein 3) (IAP-3) (rIAP-3) (rIAP3) (X-linked inhibitor of apoptosis protein) (X-linked IAP) Xiap Api3 Birc4 Rattus norvegicus (Rat) 496
A5D8Q0 XIAP_XENLA Baculoviral IAP repeat-containing protein 4 (EC 6.3.2.-) (E3 ubiquitin-protein ligase XIAP) (X-linked inhibitor of apoptosis protein) (X-linked IAP) (xXIAP) xiap birc4 Xenopus laevis (African clawed frog) 488
Q5BKL8 XIAP_XENTR Baculoviral IAP repeat-containing protein 4 (EC 6.3.2.-) (E3 ubiquitin-protein ligase XIAP) (X-linked inhibitor of apoptosis protein) (X-linked IAP) xiap birc4 Xenopus tropicalis (Western clawed frog) (Silurana tropicalis) 492
Q9NR28 DBLOH_HUMAN Diablo homolog; mitochondrial (Direct IAP-binding protein with low pI) (Second mitochondria-derived activator of caspase) (Smac) DIABLO SMAC Homo sapiens (Human) 239
Q9JIQ3 DBLOH_MOUSE Diablo homolog; mitochondrial (Direct IAP-binding protein with low pI) (Second mitochondria-derived activator of caspase) (Smac) Diablo Smac Mus musculus (Mouse) 237
Q5RBH2 DBLOH_PONAB Diablo homolog; mitochondrial DIABLO Pongo abelii (Sumatran orangutan) 239
A4GZV0 DBLOH_XENLA Diablo homolog; mitochondrial (Direct IAP-binding protein with low pI) (Second mitochondria-derived activator of caspase) (Smac protein) (XSmac) diablo smac Xenopus laevis (African clawed frog) 244
Q0IJ31 DBLOH_XENTR Diablo homolog; mitochondrial (Direct IAP-binding protein with low pI) (Second mitochondria-derived activator of caspase) (Smac protein) diablo smac Xenopus tropicalis (Western clawed frog) (Silurana tropicalis) 244
P98170 XIAP_HUMAN Baculoviral IAP repeat-containing protein 4 (EC 6.3.2.-) (E3 ubiquitin-protein ligase XIAP) (IAP-like protein) (ILP) (hILP) (Inhibitor of apoptosis protein 3) (IAP-3) (hIAP-3) (hIAP3) (X-linked inhibitor of apoptosis protein) (X-linked IAP) XIAP API3 BIRC4 IAP3 Homo sapiens (Human) 497

Small molecules tested in XIAP binding assays:

566 datapoints for 319 distinct small molecules


Name Embelin
Affinity IC50 (FP) 4uM
Assay description Fluorencence Polarisation assay; Smac peptides fluorescent label
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://dx.doi.org/10.1021/jm030420+
Doc title Discovery of embelin as a cell-permeable, small-molecular weight inhibitor of XIAP through structure-based computational screening of a traditional herbal medicine three-dimensional structure database.
PDB None

Name EmbelinDev_6a
Affinity Ki (FP) 10uM
Assay description Fluorencence Polarisation assay; Smac peptides fluorescent label
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://dx.doi.org/10.1016/j.bmcl.2006.08.072
Doc title Design, synthesis, and characterization of new embelin derivatives as potent inhibitors of X-linked inhibitor of apoptosis protein.
PDB None

Name EmbelinDev_6d
Affinity Ki (FP) 700nM
Assay description Fluorencence Polarisation assay; Smac peptides fluorescent label
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://dx.doi.org/10.1016/j.bmcl.2006.08.072
Doc title Design, synthesis, and characterization of new embelin derivatives as potent inhibitors of X-linked inhibitor of apoptosis protein.
PDB None

Name SmacLike_1
Affinity Kd (FP) 12nM
Assay description Fluorencence Polarisation assay; Smac peptides fluorescent label
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://dx.doi.org/10.1021/jm040037k
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB 1TFQ - (998)

Name SmacLike_2
Affinity Kd (FP) 5nM
Assay description Fluorencence Polarisation assay; Smac peptides fluorescent label
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://dx.doi.org/10.1021/jm040037k
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB 1TFT - (997)

Name JMC51_21
Affinity Ki (FP) 0.067 +- 0.018 uM
Assay description Fluorencence Polarisation assay; Smac peptides fluorescent label
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://dx.doi.org/10.1021/jm8006849
Doc title Structure-based design, synthesis, evaluation, and crystallographic studies of conformationally constrained Smac mimetics as inhibitors of the X-linked inhibitor of apoptosis protein (XIAP).
PDB 2JK7 - (BI6)

Name Smac005
Affinity IC50 FP 270 +- 20 nM
Assay description Fluorencence Polarisation assay; Smac peptides fluorescent label
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://dx.doi.org/10.1016/j.jmb.2008.09.064
Doc title Targeting the X-linked inhibitor of apoptosis protein through 4-substituted azabicyclo[5.3.0]alkane smac mimetics. Structure, activity, and recognition principles.
PDB 3CM7 - (X22)

Name Smac005
Affinity IC50 FP 270 +- 20 nM
Assay description Fluorencence Polarisation assay; Smac peptides fluorescent label
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://dx.doi.org/10.1016/j.jmb.2008.09.064
Doc title Targeting the X-linked inhibitor of apoptosis protein through 4-substituted azabicyclo[5.3.0]alkane smac mimetics. Structure, activity, and recognition principles.
PDB 3CLX - (X22)

Name Smac010
Affinity IC50 FP 970 +- 120 nM
Assay description Fluorencence Polarisation assay; Smac peptides fluorescent label
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://dx.doi.org/10.1016/j.jmb.2008.09.064
Doc title Targeting the X-linked inhibitor of apoptosis protein through 4-substituted azabicyclo[5.3.0]alkane smac mimetics. Structure, activity, and recognition principles.
PDB 3CM2 - (X23)

Name CHEMBL1230662
Affinity Kd = 0.01uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB 1TFQ - (998)

Name CHEMBL1241424
Affinity IC50 = 361nM
Assay description Displacement of fluorescent SM5F peptide from His-tagged human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20684551
Doc title Nonpeptidic and potent small-molecule inhibitors of cIAP-1/2 and XIAP proteins.
PDB None

Name CHEMBL1241424
Affinity Ki = 108nM
Assay description Displacement of fluorescent SM5F peptide from His-tagged human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20684551
Doc title Nonpeptidic and potent small-molecule inhibitors of cIAP-1/2 and XIAP proteins.
PDB None

Name CHEMBL1241425
Affinity Ki = 305.2nM
Assay description Displacement of fluorescent SM5F peptide from His-tagged human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20684551
Doc title Nonpeptidic and potent small-molecule inhibitors of cIAP-1/2 and XIAP proteins.
PDB None

Name CHEMBL1241425
Affinity IC50 = 1017nM
Assay description Displacement of fluorescent SM5F peptide from His-tagged human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20684551
Doc title Nonpeptidic and potent small-molecule inhibitors of cIAP-1/2 and XIAP proteins.
PDB None

Name CHEMBL1241426
Affinity IC50 = 125nM
Assay description Displacement of fluorescent SM5F peptide from His-tagged human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20684551
Doc title Nonpeptidic and potent small-molecule inhibitors of cIAP-1/2 and XIAP proteins.
PDB None

Name CHEMBL1241426
Affinity Ki = 36nM
Assay description Displacement of fluorescent SM5F peptide from His-tagged human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20684551
Doc title Nonpeptidic and potent small-molecule inhibitors of cIAP-1/2 and XIAP proteins.
PDB None

Name CHEMBL1242922
Affinity Ki = 330.6nM
Assay description Displacement of fluorescent SM5F peptide from His-tagged human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20684551
Doc title Nonpeptidic and potent small-molecule inhibitors of cIAP-1/2 and XIAP proteins.
PDB None

Name CHEMBL1242922
Affinity IC50 = 1102nM
Assay description Displacement of fluorescent SM5F peptide from His-tagged human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20684551
Doc title Nonpeptidic and potent small-molecule inhibitors of cIAP-1/2 and XIAP proteins.
PDB None

Name CHEMBL1243385
Affinity IC50 = 1068nM
Assay description Displacement of fluorescent SM5F peptide from His-tagged human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20684551
Doc title Nonpeptidic and potent small-molecule inhibitors of cIAP-1/2 and XIAP proteins.
PDB None

Name CHEMBL1243385
Affinity Ki = 320.3nM
Assay description Displacement of fluorescent SM5F peptide from His-tagged human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20684551
Doc title Nonpeptidic and potent small-molecule inhibitors of cIAP-1/2 and XIAP proteins.
PDB None

Name CHEMBL150
Affinity IC50 > 100uM
Assay description Displacement of fluorescent SM5F peptide from XIAP linker BIR3 domain after 3 hrs by fluorescence polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21087868
Doc title In silico discovery of acylated flavonol monorhamnosides from Eriobotrya japonica as natural, small-molecular weight inhibitors of XIAP BIR3.
PDB None

Name CHEMBL1616828
Affinity Ki = 0.66uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1616828
Affinity Ki = 8.06uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1617609
Affinity Ki = 4.41uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1617609
Affinity Ki = 0.8uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1617658
Affinity Ki = 4.07uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1617658
Affinity Ki = 1.4uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1617726
Affinity Ki = 1.91uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1617726
Affinity Ki = 12.71uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1617727
Affinity Ki = 0.65uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1617727
Affinity Ki = 2.33uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1618026
Affinity Ki = 26.15uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1618026
Affinity Ki = 20.07uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1618706
Affinity Ki = 1.5uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1618706
Affinity Ki = 1.29uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1619739
Affinity Ki = 0.54uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1619739
Affinity Ki = 1.29uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1619777
Affinity Ki > 39uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1619777
Affinity Ki > 56uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1620854
Affinity Ki = 9.7uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1620854
Affinity Ki = 5.62uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1620862
Affinity Ki = 0.35uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1620862
Affinity Ki = 1.67uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1620893
Affinity Ki = 0.7uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1620893
Affinity Ki = 3.12uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1621001
Affinity Ki = 4.94uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1621001
Affinity Ki = 13.78uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1621745
Affinity Ki = 0.59uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1621745
Affinity Ki = 3.36uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1621840
Affinity Ki = 37.06uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1621840
Affinity Ki = 6.07uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1621842
Affinity Ki = 0.055uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1621842
Affinity Ki = 1.37uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1621847
Affinity Ki = 2.55uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1621847
Affinity Ki = 16.21uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1622024
Affinity Ki = 0.12uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1622024
Affinity Ki = 2.01uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1622564
Affinity Ki = 0.42uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1622564
Affinity Ki = 0.99uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1622682
Affinity Ki = 7.2uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1622682
Affinity Ki = 56.13uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1622728
Affinity Ki = 6.1uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1622728
Affinity Ki = 4.75uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1623521
Affinity Ki = 1.4uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1623521
Affinity Ki = 4.97uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1623582
Affinity Ki = 5.5uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1623582
Affinity Ki = 0.74uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1624713
Affinity Ki = 0.44uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1624713
Affinity Ki = 1.51uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1625066
Affinity Ki = 1.08uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1625066
Affinity Ki = 0.39uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1625398
Affinity Ki > 39uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1625398
Affinity Ki > 56uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1625449
Affinity Ki = 10.93uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1625449
Affinity Ki = 8.18uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1642586
Affinity IC50 > 10.4uM
Assay description Displacement of fluorescent SM5F peptide from XIAP linker BIR3 domain after 3 hrs by fluorescence polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21087868
Doc title In silico discovery of acylated flavonol monorhamnosides from Eriobotrya japonica as natural, small-molecular weight inhibitors of XIAP BIR3.
PDB None

Name CHEMBL1672168
Affinity IC50 = 280nM
Assay description Inhibition of XIAP by FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672169
Affinity Ki = 270nM
Assay description Inhibition of XIAP by FP assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672259
Affinity Activity = 100uM
Assay description Inhibition of XIAP at 100 uM
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672260
Affinity Kd = 31nM
Assay description Inhibition of XIAP by FP assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672261
Affinity INH = 16.7%
Assay description Inhibition of XIAP-Bir3 domain at 10 uM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672261
Affinity INH = 15.8%
Assay description Inhibition of XIAP-Bir3 domain at 10 uM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672261
Affinity INH = 97.1%
Assay description Inhibition of XIAP-Bir3 domain at 100 uM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672261
Affinity INH = 83.2%
Assay description Inhibition of XIAP-Bir3 domain at 100 uM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672261
Affinity INH = 67.4%
Assay description Inhibition of XIAP-Bir3 domain at 10 uM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672261
Affinity INH = 83.6%
Assay description Inhibition of XIAP-Bir3 domain at 100 uM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672262
Affinity INH = 3.6%
Assay description Inhibition of XIAP-Bir3 domain at 100 nM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672262
Affinity INH = 23.6%
Assay description Inhibition of XIAP-Bir3 domain at 1 uM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672262
Affinity Kd = 21.6uM
Assay description Inhibition of XIAP-Bir3 domain by calorimetric titration assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672262
Affinity INH = 77.2%
Assay description Inhibition of XIAP-Bir3 domain at 10 uM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672262
Affinity INH = 96.9%
Assay description Inhibition of XIAP-Bir3 domain at 100 uM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672262
Affinity Kd = 27.7uM
Assay description Inhibition of XIAP-Bir3 domain by NMR titration
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672263
Affinity INH = 82.5%
Assay description Inhibition of XIAP-Bir3 domain at 100 uM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672263
Affinity INH = 15.6%
Assay description Inhibition of XIAP-Bir3 domain at 10 uM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672264
Affinity INH = 23.4%
Assay description Inhibition of XIAP-Bir3 domain at 100 uM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672264
Affinity INH = 11.1%
Assay description Inhibition of XIAP-Bir3 domain at 1 uM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672264
Affinity INH = 19.9%
Assay description Inhibition of XIAP-Bir3 domain at 10 uM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672265
Affinity INH = 12.3%
Assay description Inhibition of XIAP-Bir3 domain at 1 uM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672265
Affinity INH = 97.2%
Assay description Inhibition of XIAP-Bir3 domain at 100 uM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672265
Affinity INH = 9.1%
Assay description Inhibition of XIAP-Bir3 domain at 100 nM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672265
Affinity INH = 58%
Assay description Inhibition of XIAP-Bir3 domain at 10 uM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672266
Affinity INH = 10.8%
Assay description Inhibition of XIAP-Bir3 domain at 1 uM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672266
Affinity INH = 20.7%
Assay description Inhibition of XIAP-Bir3 domain at 100 uM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL1672266
Affinity INH = 15%
Assay description Inhibition of XIAP-Bir3 domain at 10 uM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL178103
Affinity Kd = 21uM
Assay description Dissociation constant against BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664855
Doc title Non-peptidic small molecule inhibitors of XIAP.
PDB None

Name CHEMBL179800
Affinity Kd = 7.1uM
Assay description Dissociation constant against BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664855
Doc title Non-peptidic small molecule inhibitors of XIAP.
PDB None

Name CHEMBL179951
Affinity Kd = 4.8uM
Assay description Dissociation constant against BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664855
Doc title Non-peptidic small molecule inhibitors of XIAP.
PDB None

Name CHEMBL1800078
Affinity Ki = 0.44uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1800078
Affinity Ki = 1.84uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1800335
Affinity Ki = 3.58uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1800335
Affinity Ki = 0.66uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1800336
Affinity Ki = 1.05uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1800336
Affinity Ki = 9.07uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1800337
Affinity Ki > 56uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL1800337
Affinity Ki = 29.88uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL180204
Affinity Ki = 0.028uM
Assay description Binding affinity towards BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct protein complex subunits assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664859
Doc title Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics.
PDB None

Name CHEMBL180204
Affinity Ki = 1.36uM
Assay description Competitive inhibition of XIAP BIR2 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL180204
Affinity Ki = 0.25uM
Assay description Competitive inhibition of XIAP BIR3 domain by fluorescent polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21680182
Doc title Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
PDB None

Name CHEMBL180306
Affinity Ki = 13.4uM
Assay description Binding affinity towards BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct protein complex subunits assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664859
Doc title Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics.
PDB None

Name CHEMBL180350
Affinity Kd > 100uM
Assay description Dissociation constant against BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664855
Doc title Non-peptidic small molecule inhibitors of XIAP.
PDB None

Name CHEMBL180555
Affinity Kd = 4.1uM
Assay description Dissociation constant against BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664855
Doc title Non-peptidic small molecule inhibitors of XIAP.
PDB None

Name CHEMBL1807163
Affinity Active
Assay description Inhibition of human GST-tagged XIAP binding to active human caspase-3 at 3 uM after 1 hrs by GST pull-down assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21696964
Doc title Generation of Unnatural Natural Product library and identification of a small molecule inhibitor of XIAP.
PDB None

Name CHEMBL1807163
Affinity Active
Assay description Inhibition of human recombinant GST tagged XIAP expressed in Escherichia coli assessed as restoration of XIAP-mediated suppression of caspase-3 activity after 1 hrs using fluorogenic tetrapeptide Ac-DEVD-AFC substrate by caspase de-repression assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21696964
Doc title Generation of Unnatural Natural Product library and identification of a small molecule inhibitor of XIAP.
PDB None

Name CHEMBL180741
Affinity Kd = 30uM
Assay description Dissociation constant against BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664855
Doc title Non-peptidic small molecule inhibitors of XIAP.
PDB None

Name CHEMBL180747
Affinity Kd = 25uM
Assay description Dissociation constant against BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664855
Doc title Non-peptidic small molecule inhibitors of XIAP.
PDB None

Name CHEMBL180851
Affinity Kd = 20uM
Assay description Dissociation constant against BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664855
Doc title Non-peptidic small molecule inhibitors of XIAP.
PDB None

Name CHEMBL181003
Affinity Ki = 0.18uM
Assay description Binding affinity towards BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct protein complex subunits assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664859
Doc title Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics.
PDB None

Name CHEMBL181182
Affinity Ki = 68uM
Assay description Binding affinity towards BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct protein complex subunits assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664859
Doc title Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics.
PDB None

Name CHEMBL181479
Affinity Ki = 0.024uM
Assay description Binding affinity towards BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct protein complex subunits assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664859
Doc title Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics.
PDB None

Name CHEMBL181524
Affinity Kd = 15uM
Assay description Dissociation constant against BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664855
Doc title Non-peptidic small molecule inhibitors of XIAP.
PDB None

Name CHEMBL181711
Affinity Kd = 1.1uM
Assay description Dissociation constant against BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664855
Doc title Non-peptidic small molecule inhibitors of XIAP.
PDB None

Name CHEMBL181796
Affinity Kd = 5.6uM
Assay description Dissociation constant against BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664855
Doc title Non-peptidic small molecule inhibitors of XIAP.
PDB None

Name CHEMBL181872
Affinity Kd < 10uM
Assay description Inhibition of XIAP by NMR assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL181872
Affinity Kd = 0.74uM
Assay description Dissociation constant against BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664855
Doc title Non-peptidic small molecule inhibitors of XIAP.
PDB None

Name CHEMBL181872
Affinity Kd = 750nM
Assay description Inhibition of XIAP by FP assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL182034
Affinity Ki = 0.22uM
Assay description Binding affinity towards BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct protein complex subunits assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664859
Doc title Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics.
PDB None

Name CHEMBL182159
Affinity Ki = 1.2uM
Assay description Binding affinity towards BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct protein complex subunits assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664859
Doc title Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics.
PDB None

Name CHEMBL183992
Affinity Kd = 5uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL183992
Affinity Kd = 0.04uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL183992
Affinity Kd = 1.8uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL183992
Affinity Kd > 20uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL184046
Affinity Kd = 0.04uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL185928
Affinity Kd = 0.3uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL185940
Affinity Kd > 0.5uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL186265
Affinity Kd > 20uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL186287
Affinity Kd > 1uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL186319
Affinity Kd > 20uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL186717
Affinity Kd = 0.97uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL186755
Affinity Kd = 0.12uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL186819
Affinity Kd = 0.9uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL186839
Affinity Kd = 0.28uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL186871
Affinity Kd > 1uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL186911
Affinity Kd = 0.12uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL186911
Affinity Kd = 0.09uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL187005
Affinity Kd = 0.04uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL187099
Affinity Kd > 20uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL188350
Affinity Kd = 0.6uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL188508
Affinity Kd = 2.7uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL188510
Affinity Kd = 0.006uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL188726
Affinity Kd = 0.09uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL188934
Affinity Kd = 0.29uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL189071
Affinity Kd = 0.16uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL189074
Affinity Kd > 20uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL189145
Affinity Kd > 20uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL189145
Affinity Kd = 0.06uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL189145
Affinity Kd = 0.06uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL189145
Affinity Kd = 0.06uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL189145
Affinity Kd = 0.8uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL189145
Affinity Kd = 0.06uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL189202
Affinity Kd = 0.9uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL189768
Affinity Kd > 1uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL1938613
Affinity IC50 = 0.65uM
Assay description Displacement of fluorescent H-Abu-Arg-Pro-Phe-Lys-NH-FAM-NH2 peptide from XIAP BIR3 domain by fluorescence polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21664815
Doc title DNA-instructed acyl transfer reactions for the synthesis of bioactive peptides.
PDB None

Name CHEMBL1950720
Affinity Kd = 0.9uM
Assay description Binding affinity to GST-tagged BIR3 domain of XIAP by isothermal titration calorimetry
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22264476
Doc title Discovery of aminopiperidine-based Smac mimetics as IAP antagonists.
PDB None

Name CHEMBL1950864
Affinity Kd = 0.9uM
Assay description Binding affinity to GST-tagged BIR3 domain of XIAP by isothermal titration calorimetry
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22264476
Doc title Discovery of aminopiperidine-based Smac mimetics as IAP antagonists.
PDB None

Name CHEMBL1957013
Affinity IC50 = 58nM
Assay description Displacement of AbuRPF-K(5-Fam)-NH2 from recombinant human His-tagged-XIAP BIR3 domain after 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22342627
Doc title Rational design, synthesis and characterization of potent, drug-like monomeric Smac mimetics as pro-apoptotic anticancer agents.
PDB None

Name CHEMBL1957014
Affinity IC50 = 52nM
Assay description Displacement of AbuRPF-K(5-Fam)-NH2 from recombinant human His-tagged-XIAP BIR3 domain after 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22342627
Doc title Rational design, synthesis and characterization of potent, drug-like monomeric Smac mimetics as pro-apoptotic anticancer agents.
PDB None

Name CHEMBL1957015
Affinity IC50 = 57nM
Assay description Displacement of AbuRPF-K(5-Fam)-NH2 from recombinant human His-tagged-XIAP BIR3 domain after 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22342627
Doc title Rational design, synthesis and characterization of potent, drug-like monomeric Smac mimetics as pro-apoptotic anticancer agents.
PDB None

Name CHEMBL1957016
Affinity IC50 = 78nM
Assay description Displacement of AbuRPF-K(5-Fam)-NH2 from recombinant human His-tagged-XIAP BIR3 domain after 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22342627
Doc title Rational design, synthesis and characterization of potent, drug-like monomeric Smac mimetics as pro-apoptotic anticancer agents.
PDB None

Name CHEMBL1957017
Affinity IC50 = 47nM
Assay description Displacement of AbuRPF-K(5-Fam)-NH2 from recombinant human His-tagged-XIAP BIR3 domain after 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22342627
Doc title Rational design, synthesis and characterization of potent, drug-like monomeric Smac mimetics as pro-apoptotic anticancer agents.
PDB None

Name CHEMBL1957018
Affinity IC50 = 47nM
Assay description Displacement of AbuRPF-K(5-Fam)-NH2 from recombinant human His-tagged-XIAP BIR3 domain after 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22342627
Doc title Rational design, synthesis and characterization of potent, drug-like monomeric Smac mimetics as pro-apoptotic anticancer agents.
PDB None

Name CHEMBL1957019
Affinity IC50 = 53nM
Assay description Displacement of AbuRPF-K(5-Fam)-NH2 from recombinant human His-tagged-XIAP BIR3 domain after 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22342627
Doc title Rational design, synthesis and characterization of potent, drug-like monomeric Smac mimetics as pro-apoptotic anticancer agents.
PDB None

Name CHEMBL1957020
Affinity IC50 = 44nM
Assay description Displacement of AbuRPF-K(5-Fam)-NH2 from recombinant human His-tagged-XIAP BIR3 domain after 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22342627
Doc title Rational design, synthesis and characterization of potent, drug-like monomeric Smac mimetics as pro-apoptotic anticancer agents.
PDB None

Name CHEMBL1957021
Affinity IC50 = 41nM
Assay description Displacement of AbuRPF-K(5-Fam)-NH2 from recombinant human His-tagged-XIAP BIR3 domain after 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22342627
Doc title Rational design, synthesis and characterization of potent, drug-like monomeric Smac mimetics as pro-apoptotic anticancer agents.
PDB None

Name CHEMBL1957022
Affinity IC50 = 198nM
Assay description Displacement of AbuRPF-K(5-Fam)-NH2 from recombinant human His-tagged-XIAP BIR3 domain after 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22342627
Doc title Rational design, synthesis and characterization of potent, drug-like monomeric Smac mimetics as pro-apoptotic anticancer agents.
PDB None

Name CHEMBL1957023
Affinity IC50 = 65nM
Assay description Displacement of AbuRPF-K(5-Fam)-NH2 from recombinant human His-tagged-XIAP BIR3 domain after 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22342627
Doc title Rational design, synthesis and characterization of potent, drug-like monomeric Smac mimetics as pro-apoptotic anticancer agents.
PDB None

Name CHEMBL1957024
Affinity IC50 = 111nM
Assay description Displacement of AbuRPF-K(5-Fam)-NH2 from recombinant human His-tagged-XIAP BIR3 domain after 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22342627
Doc title Rational design, synthesis and characterization of potent, drug-like monomeric Smac mimetics as pro-apoptotic anticancer agents.
PDB None

Name CHEMBL1957025
Affinity IC50 = 181nM
Assay description Displacement of AbuRPF-K(5-Fam)-NH2 from recombinant human His-tagged-XIAP BIR3 domain after 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22342627
Doc title Rational design, synthesis and characterization of potent, drug-like monomeric Smac mimetics as pro-apoptotic anticancer agents.
PDB None

Name CHEMBL1957026
Affinity IC50 = 57nM
Assay description Displacement of AbuRPF-K(5-Fam)-NH2 from recombinant human His-tagged-XIAP BIR3 domain after 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22342627
Doc title Rational design, synthesis and characterization of potent, drug-like monomeric Smac mimetics as pro-apoptotic anticancer agents.
PDB None

Name CHEMBL1957105
Affinity IC50 = 58nM
Assay description Displacement of AbuRPF-K(5-Fam)-NH2 from recombinant human His-tagged-XIAP BIR3 domain after 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22342627
Doc title Rational design, synthesis and characterization of potent, drug-like monomeric Smac mimetics as pro-apoptotic anticancer agents.
PDB None

Name CHEMBL1957106
Affinity IC50 = 57nM
Assay description Displacement of AbuRPF-K(5-Fam)-NH2 from recombinant human His-tagged-XIAP BIR3 domain after 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22342627
Doc title Rational design, synthesis and characterization of potent, drug-like monomeric Smac mimetics as pro-apoptotic anticancer agents.
PDB None

Name CHEMBL1957107
Affinity IC50 = 52nM
Assay description Displacement of AbuRPF-K(5-Fam)-NH2 from recombinant human His-tagged-XIAP BIR3 domain after 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22342627
Doc title Rational design, synthesis and characterization of potent, drug-like monomeric Smac mimetics as pro-apoptotic anticancer agents.
PDB None

Name CHEMBL2063862
Affinity Ki = 0.43uM
Assay description Displacement of 5-FAM-conjugated AVP-diPhe-FAM from XIAP BIR3 domain after 30 mins by fluorescence polarization-based competition assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22413863
Doc title Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
PDB None

Name CHEMBL2063863
Affinity Ki = 0.19uM
Assay description Displacement of 5-FAM-conjugated AVP-diPhe-FAM from XIAP BIR3 domain after 30 mins by fluorescence polarization-based competition assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22413863
Doc title Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
PDB None

Name CHEMBL2063864
Affinity Ki = 7.6uM
Assay description Displacement of 5-FAM-conjugated AVP-diPhe-FAM from XIAP BIR3 domain after 30 mins by fluorescence polarization-based competition assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22413863
Doc title Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
PDB None

Name CHEMBL2063865
Affinity Ki = 0.8uM
Assay description Displacement of 5-FAM-conjugated AVP-diPhe-FAM from XIAP BIR3 domain after 30 mins by fluorescence polarization-based competition assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22413863
Doc title Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
PDB None

Name CHEMBL2063866
Affinity Ki = 0.41uM
Assay description Displacement of 5-FAM-conjugated AVP-diPhe-FAM from XIAP BIR3 domain after 30 mins by fluorescence polarization-based competition assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22413863
Doc title Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
PDB None

Name CHEMBL2063867
Affinity Ki = 0.7uM
Assay description Displacement of 5-FAM-conjugated AVP-diPhe-FAM from XIAP BIR3 domain after 30 mins by fluorescence polarization-based competition assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22413863
Doc title Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
PDB None

Name CHEMBL2063868
Affinity Ki = 0.035uM
Assay description Displacement of 5-FAM-conjugated AVP-diPhe-FAM from XIAP BIR3 domain after 30 mins by fluorescence polarization-based competition assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22413863
Doc title Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
PDB None

Name CHEMBL2063869
Affinity Ki = 0.112uM
Assay description Displacement of 5-FAM-conjugated AVP-diPhe-FAM from XIAP BIR2 domain after 30 mins by fluorescence polarization-based competition assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22413863
Doc title Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
PDB None

Name CHEMBL2063869
Affinity Active
Assay description Inhibition of Flag-tagged XIAP BIR3 domain binding to cIAP2 expressed in human HEK293T cells at 1 to 50 uM after 2 hrs by immunoprecipitation
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22413863
Doc title Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
PDB None

Name CHEMBL2063869
Affinity Ki = 0.028uM
Assay description Displacement of 5-FAM-conjugated AVP-diPhe-FAM from XIAP BIR3 domain after 30 mins by fluorescence polarization-based competition assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22413863
Doc title Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
PDB None

Name CHEMBL2063869
Affinity Active
Assay description Inhibition of Flag-tagged XIAP BIR3 domain binding to cIAP1 expressed in human HEK293T cells at 1 to 50 uM after 2 hrs by immunoprecipitation
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22413863
Doc title Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
PDB None

Name CHEMBL2063869
Affinity Active
Assay description Inhibition of Flag-tagged XIAP BIR3 domain binding to caspase-9 expressed in human HEK293T cells at 1 to 100 uM after 2 hrs by immunoprecipitation
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22413863
Doc title Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
PDB None

Name CHEMBL2063869
Affinity Active
Assay description Inhibition of Flag-tagged XIAP BIR3 domain binding to ML-IAP expressed in human HEK293T cells at 1 to 50 uM after 2 hrs by immunoprecipitation
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22413863
Doc title Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
PDB None

Name CHEMBL2096803
Affinity Kd = 0.7uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB 1TFQ - (998)

Name CHEMBL2096803
Affinity Kd > 1uM
Assay description Binding affinity to the BIR3 Domain of XIAP
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB 1TFQ - (998)

Name CHEMBL2158051
Affinity Ki = 66.4nM
Assay description Competitive inhibition of human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) after 2 to 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21443232
Doc title A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
PDB None

Name CHEMBL2158051
Affinity IC50 = 225nM
Assay description Competitive inhibition of human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) after 2 to 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21443232
Doc title A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
PDB None

Name CHEMBL2158052
Affinity Ki = 67300nM
Assay description Competitive inhibition of human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) after 2 to 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21443232
Doc title A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
PDB None

Name CHEMBL2158052
Affinity IC50 = 221000nM
Assay description Competitive inhibition of human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) after 2 to 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21443232
Doc title A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
PDB None

Name CHEMBL2158053
Affinity Active
Assay description Binding affinity to cIAP1 in human MDA-MB-231 cells after 30 mins in presence of SM-428 by biotin-streptavidin-pull-down assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21443232
Doc title A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
PDB None

Name CHEMBL2158053
Affinity Dose-dependent effect
Assay description Binding affinity to XIAP in human MDA-MB-231 cells after 30 mins by biotin-streptavidin-pull-down assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21443232
Doc title A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
PDB None

Name CHEMBL2158053
Affinity Dose-dependent effect
Assay description Binding affinity to XIAP in human MDA-MB-231 cells after 30 mins in presence of SM-406 by biotin-streptavidin-pull-down assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21443232
Doc title A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
PDB None

Name CHEMBL2158053
Affinity Ki = 25.9nM
Assay description Competitive inhibition of human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) after 2 to 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21443232
Doc title A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
PDB None

Name CHEMBL2158053
Affinity Active
Assay description Binding affinity to XIAP in human MDA-MB-231 cells after 30 mins in presence of SM-428 by biotin-streptavidin-pull-down assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21443232
Doc title A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
PDB None

Name CHEMBL2158054
Affinity Kd = 4.4nM
Assay description Binding affinity to His6-tagged human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) assessed as dissociation constant after 2 to 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21443232
Doc title A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
PDB None

Name CHEMBL218832
Affinity Ki = 0.061uM
Assay description Binding affinity to recombinant XIAP BIR3 by FP assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17181177
Doc title Design, synthesis, and evaluation of a potent, cell-permeable, conformationally constrained second mitochondria derived activator of caspase (Smac) mimetic.
PDB None

Name CHEMBL218832
Affinity Activity = 31%
Assay description Displacement of FITC-SMAC probe from human recombinant XIAP linker BIR2-BIR3 expressed in Escherichia coli BL21 by fluorescence polarization assay relative to control
-- Direct single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19620011
Doc title Rational design, synthesis and characterization of potent, non-peptidic Smac mimics/XIAP inhibitors as proapoptotic agents for cancer therapy.
PDB None

Name CHEMBL218832
Affinity IC50 = 420nM
Assay description Binding affinity to human recombinant XIAP linker BIR2-BIR3 expressed in Escherichia coli BL21 by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19620011
Doc title Rational design, synthesis and characterization of potent, non-peptidic Smac mimics/XIAP inhibitors as proapoptotic agents for cancer therapy.
PDB None

Name CHEMBL218832
Affinity Ki = 0.061uM
Assay description Binding affinity to N-terminal 6xHis-tagged human cloned XIAP BIR3 domain expressed in Escherichia coli BL21 (DE3) by fluorescence polarization-based competitive binding assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18954041
Doc title Structure-based design, synthesis, evaluation, and crystallographic studies of conformationally constrained Smac mimetics as inhibitors of the X-linked inhibitor of apoptosis protein (XIAP).
PDB None

Name CHEMBL218832
Affinity IC50 = 530nM
Assay description Binding affinity to human recombinant XIAP BIR3 domain expressed in Escherichia coli BL21 by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19620011
Doc title Rational design, synthesis and characterization of potent, non-peptidic Smac mimics/XIAP inhibitors as proapoptotic agents for cancer therapy.
PDB None

Name CHEMBL218832
Affinity Activity = 11%
Assay description Displacement of FITC-SMAC probe from human recombinant XIAP BIR3 domain expressed in Escherichia coli BL21 by fluorescence polarization assay relative to control
-- Direct single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19620011
Doc title Rational design, synthesis and characterization of potent, non-peptidic Smac mimics/XIAP inhibitors as proapoptotic agents for cancer therapy.
PDB None

Name CHEMBL219139
Affinity Ki = 14.4uM
Assay description Binding affinity to recombinant XIAP BIR3 by FP assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17181177
Doc title Design, synthesis, and evaluation of a potent, cell-permeable, conformationally constrained second mitochondria derived activator of caspase (Smac) mimetic.
PDB None

Name CHEMBL219139
Affinity Ki = 14.4uM
Assay description Binding affinity to N-terminal 6xHis-tagged human cloned XIAP BIR3 domain expressed in Escherichia coli BL21 (DE3) by fluorescence polarization-based competitive binding assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18954041
Doc title Structure-based design, synthesis, evaluation, and crystallographic studies of conformationally constrained Smac mimetics as inhibitors of the X-linked inhibitor of apoptosis protein (XIAP).
PDB None

Name CHEMBL219963
Affinity Ki = 29uM
Assay description Binding affinity to recombinant XIAP BIR3 by FP assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17181177
Doc title Design, synthesis, and evaluation of a potent, cell-permeable, conformationally constrained second mitochondria derived activator of caspase (Smac) mimetic.
PDB None

Name CHEMBL2204570
Affinity IC50 = 293nM
Assay description Displacement of FITC-Smac from human His-tagged XIAP BIR3 domain (241 to 356 residues) after 3 hrs by fluorescent polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23062821
Doc title Dimeric Smac mimetics/IAP inhibitors as in vivo-active pro-apoptotic agents. Part II: Structural and biological characterization.
PDB None

Name CHEMBL2204570
Affinity IC50 = 5.3nM
Assay description Displacement of Smac-1F from human His-tagged XIAP linker BIR2-BIR3 linker (124 to 356 residues) after 3 hrs by fluorescent polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23062821
Doc title Dimeric Smac mimetics/IAP inhibitors as in vivo-active pro-apoptotic agents. Part II: Structural and biological characterization.
PDB None

Name CHEMBL2204571
Affinity IC50 = 80.7nM
Assay description Displacement of FITC-Smac from human His-tagged XIAP BIR3 domain (241 to 356 residues) after 3 hrs by fluorescent polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23062821
Doc title Dimeric Smac mimetics/IAP inhibitors as in vivo-active pro-apoptotic agents. Part II: Structural and biological characterization.
PDB 3G76 - (CZ3)

Name CHEMBL2204571
Affinity IC50 = 3.3nM
Assay description Displacement of Smac-1F from human His-tagged XIAP linker BIR2-BIR3 linker (124 to 356 residues) after 3 hrs by fluorescent polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23062821
Doc title Dimeric Smac mimetics/IAP inhibitors as in vivo-active pro-apoptotic agents. Part II: Structural and biological characterization.
PDB 3G76 - (CZ3)

Name CHEMBL221137
Affinity IC50 = 4.1uM
Assay description Compound was tested for inhibiotry activity towards XIAP BIR3 protein
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15115387
Doc title Discovery of embelin as a cell-permeable, small-molecular weight inhibitor of XIAP through structure-based computational screening of a traditional herbal medicine three-dimensional structure database.
PDB None

Name CHEMBL221137
Affinity Ki = 0.4uM
Assay description Binding affinity to recombinant XIAP BIR3 by FP assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16962773
Doc title Design, synthesis, and characterization of new embelin derivatives as potent inhibitors of X-linked inhibitor of apoptosis protein.
PDB None

Name CHEMBL221137
Affinity IC50 = 4.1uM
Assay description Inhibitory concentration of compound against XIAP BIR3 protein
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15115387
Doc title Discovery of embelin as a cell-permeable, small-molecular weight inhibitor of XIAP through structure-based computational screening of a traditional herbal medicine three-dimensional structure database.
PDB None

Name CHEMBL221256
Affinity Ki = 0.38uM
Assay description Binding affinity to recombinant XIAP BIR3 by FP assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16962773
Doc title Design, synthesis, and characterization of new embelin derivatives as potent inhibitors of X-linked inhibitor of apoptosis protein.
PDB None

Name CHEMBL221313
Affinity Ki = 0.18uM
Assay description Binding affinity to recombinant XIAP BIR3 by FP assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16962773
Doc title Design, synthesis, and characterization of new embelin derivatives as potent inhibitors of X-linked inhibitor of apoptosis protein.
PDB None

Name CHEMBL221598
Affinity Ki = 1.25uM
Assay description Binding affinity to recombinant XIAP BIR3 by FP assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16962773
Doc title Design, synthesis, and characterization of new embelin derivatives as potent inhibitors of X-linked inhibitor of apoptosis protein.
PDB None

Name CHEMBL221599
Affinity Ki = 1.3uM
Assay description Binding affinity to recombinant XIAP BIR3 by FP assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16962773
Doc title Design, synthesis, and characterization of new embelin derivatives as potent inhibitors of X-linked inhibitor of apoptosis protein.
PDB None

Name CHEMBL221647
Affinity Ki = 0.71uM
Assay description Binding affinity to recombinant XIAP BIR3 by FP assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16962773
Doc title Design, synthesis, and characterization of new embelin derivatives as potent inhibitors of X-linked inhibitor of apoptosis protein.
PDB None

Name CHEMBL222173
Affinity Ki = 10.4uM
Assay description Binding affinity to recombinant XIAP BIR3 by FP assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16962773
Doc title Design, synthesis, and characterization of new embelin derivatives as potent inhibitors of X-linked inhibitor of apoptosis protein.
PDB None

Name CHEMBL234345
Affinity Kd = 0.5uM
Assay description Binding affinity to BIR3 domain of XIAP by competitive fluorescent binding assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17336535
Doc title Structure-activity based study of the Smac-binding pocket within the BIR3 domain of XIAP.
PDB None

Name CHEMBL234346
Affinity INH = 55.4%
Assay description Inhibition of XIAP-Bir3 domain at 500 nM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL234346
Affinity Kd = 0.04uM
Assay description Binding affinity to BIR3 domain of XIAP by competitive fluorescent binding assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17336535
Doc title Structure-activity based study of the Smac-binding pocket within the BIR3 domain of XIAP.
PDB None

Name CHEMBL234346
Affinity Kd = 0.73uM
Assay description Binding affinity to histidine6-tagged human XIAP Bir3 domain expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18956862
Doc title Fragment-based design of small molecule X-linked inhibitor of apoptosis protein inhibitors.
PDB None

Name CHEMBL234346
Affinity INH = 25.5%
Assay description Inhibition of XIAP-Bir3 domain at 100 nM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL234346
Affinity INH = 75%
Assay description Inhibition of XIAP-Bir3 domain at 1 uM by TR-FRET assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21241056
Doc title Screening multicomponent reactions for X-linked inhibitor of apoptosis-baculoviral inhibitor of apoptosis protein repeats domain binder.
PDB None

Name CHEMBL234558
Affinity Kd = 120uM
Assay description Binding affinity to BIR3 domain of XIAP by competitive fluorescent binding assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17336535
Doc title Structure-activity based study of the Smac-binding pocket within the BIR3 domain of XIAP.
PDB None

Name CHEMBL234559
Affinity Kd = 300uM
Assay description Binding affinity to BIR3 domain of XIAP by competitive fluorescent binding assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17336535
Doc title Structure-activity based study of the Smac-binding pocket within the BIR3 domain of XIAP.
PDB None

Name CHEMBL240528
Affinity IC50 > 100uM
Assay description Displacement of fluorescent SM5F peptide from XIAP linker BIR3 domain after 3 hrs by fluorescence polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21087868
Doc title In silico discovery of acylated flavonol monorhamnosides from Eriobotrya japonica as natural, small-molecular weight inhibitors of XIAP BIR3.
PDB None

Name CHEMBL359465
Affinity Kd = 30uM
Assay description Dissociation constant against BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664855
Doc title Non-peptidic small molecule inhibitors of XIAP.
PDB None

Name CHEMBL359565
Affinity Kd > 1uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL359675
Affinity Kd = 22uM
Assay description Dissociation constant against BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664855
Doc title Non-peptidic small molecule inhibitors of XIAP.
PDB None

Name CHEMBL359812
Affinity Ki = 1.27uM
Assay description Binding affinity towards BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct protein complex subunits assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664859
Doc title Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics.
PDB None

Name CHEMBL360180
Affinity Kd = 0.04uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL360545
Affinity Ki = 4.41uM
Assay description Binding affinity towards BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct protein complex subunits assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664859
Doc title Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics.
PDB None

Name CHEMBL360607
Affinity Kd = 0.03uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL360947
Affinity Kd = 4.1uM
Assay description Dissociation constant against BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664855
Doc title Non-peptidic small molecule inhibitors of XIAP.
PDB None

Name CHEMBL361282
Affinity Kd = 0.02uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL361542
Affinity Ki = 0.081uM
Assay description Binding affinity towards BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct protein complex subunits assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664859
Doc title Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics.
PDB None

Name CHEMBL362027
Affinity Ki = 54uM
Assay description Binding affinity towards BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct protein complex subunits assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664859
Doc title Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics.
PDB None

Name CHEMBL362245
Affinity Ki = 4.9uM
Assay description Binding affinity towards BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct protein complex subunits assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664859
Doc title Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics.
PDB None

Name CHEMBL362377
Affinity Kd = 2uM
Assay description Dissociation constant against BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664855
Doc title Non-peptidic small molecule inhibitors of XIAP.
PDB None

Name CHEMBL363053
Affinity Kd = 0.18uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL363529
Affinity Kd = 0.01uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL363770
Affinity Kd = 0.36uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL364157
Affinity Kd = 9.6uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL364426
Affinity Kd = 8.7uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL364943
Affinity Kd = 0.19uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL365059
Affinity Ki = 0.58uM
Assay description Binding affinity to N-terminal 6xHis-tagged human cloned XIAP BIR3 domain expressed in Escherichia coli BL21 (DE3) by fluorescence polarization-based competitive binding assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18954041
Doc title Structure-based design, synthesis, evaluation, and crystallographic studies of conformationally constrained Smac mimetics as inhibitors of the X-linked inhibitor of apoptosis protein (XIAP).
PDB None

Name CHEMBL365059
Affinity IC50 = 11584nM
Assay description Competitive inhibition of human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) after 2 to 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21443232
Doc title A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
PDB None

Name CHEMBL365059
Affinity Ki = 0.58uM
Assay description Binding affinity for the recombinant XIAP BIR3 protein in displacing a fluorescently labeled Smac peptide
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15293984
Doc title Structure-based design, synthesis, and evaluation of conformationally constrained mimetics of the second mitochondria-derived activator of caspase that target the X-linked inhibitor of apoptosis protein/caspase-9 interaction site.
PDB None

Name CHEMBL365059
Affinity Ki = 3535nM
Assay description Competitive inhibition of human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) after 2 to 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21443232
Doc title A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
PDB None

Name CHEMBL365258
Affinity Kd = 0.9uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL365298
Affinity Kd = 0.005uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB 1TFT - (997)

Name CHEMBL365304
Affinity Kd = 6.7uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL365408
Affinity Kd = 0.4uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL365430
Affinity Kd = 1.6uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL365504
Affinity Kd = 3uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL365619
Affinity Kd = 0.16uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL365676
Affinity Kd = 0.05uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL365896
Affinity Kd = 0.12uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL365896
Affinity Kd > 20uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL367347
Affinity Kd = 15uM
Assay description Dissociation constant against BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664855
Doc title Non-peptidic small molecule inhibitors of XIAP.
PDB None

Name CHEMBL369736
Affinity Ki = 0.15uM
Assay description Binding affinity towards BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct protein complex subunits assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664859
Doc title Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics.
PDB None

Name CHEMBL373766
Affinity Ki = 0.58uM
Assay description Binding affinity to recombinant XIAP BIR3 by FP assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16962773
Doc title Design, synthesis, and characterization of new embelin derivatives as potent inhibitors of X-linked inhibitor of apoptosis protein.
PDB None

Name CHEMBL375349
Affinity Activity = 7%
Assay description Displacement of FITC-SMAC probe from human recombinant XIAP BIR3 domain expressed in Escherichia coli BL21 by fluorescence polarization assay relative to control
-- Direct single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19620011
Doc title Rational design, synthesis and characterization of potent, non-peptidic Smac mimics/XIAP inhibitors as proapoptotic agents for cancer therapy.
PDB None

Name CHEMBL375349
Affinity Ki = 0.025uM
Assay description Binding affinity to recombinant XIAP BIR3 by FP assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17181177
Doc title Design, synthesis, and evaluation of a potent, cell-permeable, conformationally constrained second mitochondria derived activator of caspase (Smac) mimetic.
PDB None

Name CHEMBL375349
Affinity IC50 = 360nM
Assay description Binding affinity to human recombinant XIAP linker BIR2-BIR3 expressed in Escherichia coli BL21 by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19620011
Doc title Rational design, synthesis and characterization of potent, non-peptidic Smac mimics/XIAP inhibitors as proapoptotic agents for cancer therapy.
PDB None

Name CHEMBL375349
Affinity IC50 = 460nM
Assay description Binding affinity to human recombinant XIAP BIR3 domain expressed in Escherichia coli BL21 by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19620011
Doc title Rational design, synthesis and characterization of potent, non-peptidic Smac mimics/XIAP inhibitors as proapoptotic agents for cancer therapy.
PDB None

Name CHEMBL375349
Affinity Activity = 42%
Assay description Displacement of FITC-SMAC probe from human recombinant XIAP linker BIR2-BIR3 expressed in Escherichia coli BL21 by fluorescence polarization assay relative to control
-- Direct single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19620011
Doc title Rational design, synthesis and characterization of potent, non-peptidic Smac mimics/XIAP inhibitors as proapoptotic agents for cancer therapy.
PDB None

Name CHEMBL375349
Affinity Ki = 0.025uM
Assay description Binding affinity to N-terminal 6xHis-tagged human cloned XIAP BIR3 domain expressed in Escherichia coli BL21 (DE3) by fluorescence polarization-based competitive binding assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18954041
Doc title Structure-based design, synthesis, evaluation, and crystallographic studies of conformationally constrained Smac mimetics as inhibitors of the X-linked inhibitor of apoptosis protein (XIAP).
PDB None

Name CHEMBL375784
Affinity Ki = 0.48uM
Assay description Binding affinity to recombinant XIAP BIR3 by FP assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/16962773
Doc title Design, synthesis, and characterization of new embelin derivatives as potent inhibitors of X-linked inhibitor of apoptosis protein.
PDB None

Name CHEMBL392946
Affinity Kd = 11uM
Assay description Binding affinity to BIR3 domain of XIAP by competitive fluorescent binding assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17336535
Doc title Structure-activity based study of the Smac-binding pocket within the BIR3 domain of XIAP.
PDB None

Name CHEMBL393164
Affinity Kd = 30uM
Assay description Binding affinity to BIR3 domain of XIAP by competitive fluorescent binding assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17336535
Doc title Structure-activity based study of the Smac-binding pocket within the BIR3 domain of XIAP.
PDB 2OPY - (CO9)

Name CHEMBL425176
Affinity Kd = 3.4uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL426052
Affinity Ki = 0.29uM
Assay description Binding affinity towards BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct protein complex subunits assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664859
Doc title Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics.
PDB None

Name CHEMBL426052
Affinity Ki = 0.29uM
Assay description Binding affinity to N-terminal 6xHis-tagged human cloned XIAP BIR3 domain expressed in Escherichia coli BL21 (DE3) by fluorescence polarization-based competitive binding assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18954041
Doc title Structure-based design, synthesis, evaluation, and crystallographic studies of conformationally constrained Smac mimetics as inhibitors of the X-linked inhibitor of apoptosis protein (XIAP).
PDB None

Name CHEMBL426055
Affinity Ki = 4.15uM
Assay description Binding affinity towards BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct protein complex subunits assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664859
Doc title Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics.
PDB None

Name CHEMBL433556
Affinity Kd = 0.18uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL433803
Affinity Kd = 14uM
Assay description Dissociation constant against BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664855
Doc title Non-peptidic small molecule inhibitors of XIAP.
PDB None

Name CHEMBL434896
Affinity Kd = 1.2uM
Assay description Dissociation constant against BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664855
Doc title Non-peptidic small molecule inhibitors of XIAP.
PDB None

Name CHEMBL434901
Affinity Kd > 1uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL435497
Affinity Kd = 0.8uM
Assay description Binding affinity to the BIR3 domain of X-linked IAP
-- Homologous single protein target assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15317454
Doc title Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.
PDB None

Name CHEMBL444618
Affinity Ki = 2.45uM
Assay description Binding affinity towards BIR3 domain of X-linked IAP in fluorescence polarization anisotropy competition assay
-- Direct protein complex subunits assigned: XIAP_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/15664859
Doc title Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics.
PDB None

Name CHEMBL445214
Affinity Ki > 100uM
Assay description Binding affinity to N-terminal 6xHis-tagged human cloned XIAP BIR3 domain expressed in Escherichia coli BL21 (DE3) by fluorescence polarization-based competitive binding assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18954041
Doc title Structure-based design, synthesis, evaluation, and crystallographic studies of conformationally constrained Smac mimetics as inhibitors of the X-linked inhibitor of apoptosis protein (XIAP).
PDB None

Name CHEMBL451521
Affinity Ki = 32.87uM
Assay description Binding affinity to N-terminal 6xHis-tagged human cloned XIAP BIR3 domain expressed in Escherichia coli BL21 (DE3) by fluorescence polarization-based competitive binding assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18954041
Doc title Structure-based design, synthesis, evaluation, and crystallographic studies of conformationally constrained Smac mimetics as inhibitors of the X-linked inhibitor of apoptosis protein (XIAP).
PDB None

Name CHEMBL456216
Affinity Ki = 1.2uM
Assay description Binding affinity to XIAP-BIR3 domain by fluorescence polarization competitive assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19228017
Doc title Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold.
PDB None

Name CHEMBL456400
Affinity IC50 = 169nM
Assay description Binding affinity to BIR2-BIR3 domain of XIAP by fluorescence polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22148838
Doc title Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents.
PDB None

Name CHEMBL456400
Affinity IC50 = 14.3uM
Assay description Binding affinity to BIR2 domain of XIAP by fluorescence polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22148838
Doc title Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents.
PDB None

Name CHEMBL456400
Affinity Ki = 5.5uM
Assay description Binding affinity to BIR2 domain of XIAP by fluorescence polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22148838
Doc title Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents.
PDB None

Name CHEMBL456400
Affinity IC50 = 208nM
Assay description Binding affinity to BIR3 domain of XIAP by fluorescence polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22148838
Doc title Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents.
PDB None

Name CHEMBL456400
Affinity Ki = 51nM
Assay description Binding affinity to BIR2-BIR3 domain of XIAP by fluorescence polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22148838
Doc title Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents.
PDB None

Name CHEMBL456400
Affinity Ki = 70nM
Assay description Binding affinity to BIR3 domain of XIAP by fluorescence polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22148838
Doc title Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents.
PDB None

Name CHEMBL456418
Affinity Ki = 0.5uM
Assay description Binding affinity to XIAP-BIR3 domain by fluorescence polarization competitive assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19228017
Doc title Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold.
PDB None

Name CHEMBL457240
Affinity Ki = 1.8uM
Assay description Binding affinity to XIAP-BIR3 domain by fluorescence polarization competitive assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19228017
Doc title Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold.
PDB None

Name CHEMBL457671
Affinity Ki = 3uM
Assay description Binding affinity to XIAP-BIR3 domain by fluorescence polarization competitive assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19228017
Doc title Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold.
PDB None

Name CHEMBL458345
Affinity Ki = 1.6uM
Assay description Binding affinity to XIAP-BIR3 domain by fluorescence polarization competitive assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19228017
Doc title Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold.
PDB None

Name CHEMBL458358
Affinity Kd = 30uM
Assay description Binding affinity to histidine6-tagged human XIAP Bir3 domain expressed in Escherichia coli BL21(DE3) by fluorescence polarization displacement assay in presence of FITC-labeled SMAC peptide
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18956862
Doc title Fragment-based design of small molecule X-linked inhibitor of apoptosis protein inhibitors.
PDB None

Name CHEMBL458358
Affinity Kd = 2.5uM
Assay description Binding affinity to histidine6-tagged human XIAP Bir3 domain expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18956862
Doc title Fragment-based design of small molecule X-linked inhibitor of apoptosis protein inhibitors.
PDB None

Name CHEMBL458358
Affinity Kd = 1.2uM
Assay description Binding affinity to histidine6-tagged human XIAP Bir3 domain expressed in Escherichia coli BL21(DE3)
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18956862
Doc title Fragment-based design of small molecule X-linked inhibitor of apoptosis protein inhibitors.
PDB None

Name CHEMBL458540
Affinity Ki = 0.21uM
Assay description Binding affinity to XIAP-BIR3 domain by fluorescence polarization competitive assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19228017
Doc title Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold.
PDB None

Name CHEMBL458742
Affinity Ki = 0.11uM
Assay description Binding affinity to XIAP-BIR3 domain by fluorescence polarization competitive assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19228017
Doc title Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold.
PDB None

Name CHEMBL458791
Affinity Ki = 1200nM
Assay description Displacement of fluorescently tagged SMF5 from human cloned XIAP BIR3 expressed in Escherichia coli BL21 (DE3) by competitive fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19012392
Doc title Design, synthesis, and evaluation of tricyclic, conformationally constrained small-molecule mimetics of second mitochondria-derived activator of caspases.
PDB None

Name CHEMBL459597
Affinity Ki = 0.33uM
Assay description Binding affinity to XIAP-BIR3 domain by fluorescence polarization competitive assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19228017
Doc title Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold.
PDB None

Name CHEMBL459803
Affinity Ki = 0.16uM
Assay description Binding affinity to XIAP-BIR3 domain by fluorescence polarization competitive assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19228017
Doc title Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold.
PDB None

Name CHEMBL459805
Affinity Ki = 5.9uM
Assay description Binding affinity to XIAP-BIR3 domain by fluorescence polarization competitive assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19228017
Doc title Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold.
PDB None

Name CHEMBL460203
Affinity Ki = 1.3uM
Assay description Binding affinity to XIAP-BIR3 domain by fluorescence polarization competitive assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19228017
Doc title Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold.
PDB None

Name CHEMBL461254
Affinity Ki = 14.3uM
Assay description Binding affinity to XIAP-BIR3 domain by fluorescence polarization competitive assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19228017
Doc title Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold.
PDB None

Name CHEMBL462102
Affinity Ki = 0.49uM
Assay description Binding affinity to XIAP-BIR3 domain by fluorescence polarization competitive assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19228017
Doc title Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold.
PDB None

Name CHEMBL462310
Affinity Ki = 1.2uM
Assay description Binding affinity to XIAP-BIR3 domain by fluorescence polarization competitive assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19228017
Doc title Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold.
PDB None

Name CHEMBL469515
Affinity Ki = 4.47uM
Assay description Binding affinity to N-terminal 6xHis-tagged human cloned XIAP BIR3 domain expressed in Escherichia coli BL21 (DE3) by fluorescence polarization-based competitive binding assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18954041
Doc title Structure-based design, synthesis, evaluation, and crystallographic studies of conformationally constrained Smac mimetics as inhibitors of the X-linked inhibitor of apoptosis protein (XIAP).
PDB None

Name CHEMBL469951
Affinity Ki = 43.11uM
Assay description Binding affinity to N-terminal 6xHis-tagged human cloned XIAP BIR3 domain expressed in Escherichia coli BL21 (DE3) by fluorescence polarization-based competitive binding assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18954041
Doc title Structure-based design, synthesis, evaluation, and crystallographic studies of conformationally constrained Smac mimetics as inhibitors of the X-linked inhibitor of apoptosis protein (XIAP).
PDB None

Name CHEMBL471827
Affinity Ki = 0.1uM
Assay description Binding affinity to N-terminal 6xHis-tagged human cloned XIAP BIR3 domain expressed in Escherichia coli BL21 (DE3) by fluorescence polarization-based competitive binding assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18954041
Doc title Structure-based design, synthesis, evaluation, and crystallographic studies of conformationally constrained Smac mimetics as inhibitors of the X-linked inhibitor of apoptosis protein (XIAP).
PDB None

Name CHEMBL472048
Affinity Ki = 2.33uM
Assay description Binding affinity to N-terminal 6xHis-tagged human cloned XIAP BIR3 domain expressed in Escherichia coli BL21 (DE3) by fluorescence polarization-based competitive binding assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18954041
Doc title Structure-based design, synthesis, evaluation, and crystallographic studies of conformationally constrained Smac mimetics as inhibitors of the X-linked inhibitor of apoptosis protein (XIAP).
PDB None

Name CHEMBL472254
Affinity Ki = 0.35uM
Assay description Binding affinity to N-terminal 6xHis-tagged human cloned XIAP BIR3 domain expressed in Escherichia coli BL21 (DE3) by fluorescence polarization-based competitive binding assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18954041
Doc title Structure-based design, synthesis, evaluation, and crystallographic studies of conformationally constrained Smac mimetics as inhibitors of the X-linked inhibitor of apoptosis protein (XIAP).
PDB None

Name CHEMBL472832
Affinity Ki = 31nM
Assay description Displacement of fluorescent SM5F peptide from His-tagged human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19138149
Doc title Design, synthesis, and evaluation of potent, nonpeptidic mimetics of second mitochondria-derived activator of caspases.
PDB None

Name CHEMBL475670
Affinity Ki = 3.9nM
Assay description Displacement of fluorescent SM5F peptide from His-tagged human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19138149
Doc title Design, synthesis, and evaluation of potent, nonpeptidic mimetics of second mitochondria-derived activator of caspases.
PDB None

Name CHEMBL479725
Affinity Ki = 0.57uM
Assay description Binding affinity to XIAP-BIR3 domain by fluorescence polarization competitive assay
-- Homologous single protein target assigned: XIAP_HUMAN (Intermediate curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19228017
Doc title Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold.
PDB None

Name CHEMBL481213
Affinity Ki = 14nM
Assay description Displacement of fluorescent SM5F peptide from His-tagged human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19138149
Doc title Design, synthesis, and evaluation of potent, nonpeptidic mimetics of second mitochondria-derived activator of caspases.
PDB None

Name CHEMBL481421
Affinity Ki = 209nM
Assay description Displacement of fluorescent SM5F peptide from His-tagged human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19138149
Doc title Design, synthesis, and evaluation of potent, nonpeptidic mimetics of second mitochondria-derived activator of caspases.
PDB None

Name CHEMBL481422
Affinity IC50 = 1240nM
Assay description Competitive inhibition of human XIAP linker BIR2-BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21462933
Doc title Potent bivalent Smac mimetics: effect of the linker on binding to inhibitor of apoptosis proteins (IAPs) and anticancer activity.
PDB None

Name CHEMBL481422
Affinity Ki = 0.026uM
Assay description Binding affinity to N-terminal 6xHis-tagged human cloned XIAP BIR3 domain expressed in Escherichia coli BL21 (DE3) by fluorescence polarization-based competitive binding assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18954041
Doc title Structure-based design, synthesis, evaluation, and crystallographic studies of conformationally constrained Smac mimetics as inhibitors of the X-linked inhibitor of apoptosis protein (XIAP).
PDB None

Name CHEMBL481422
Affinity Ki = 408nM
Assay description Binding affinity to BIR2-BIR3 domain of XIAP by fluorescence polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22148838
Doc title Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents.
PDB None

Name CHEMBL481422
Affinity IC50 = 819nM
Assay description Competitive inhibition of His-tagged human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) after 2 to 3 hrs by fluorescence polarization assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21462933
Doc title Potent bivalent Smac mimetics: effect of the linker on binding to inhibitor of apoptosis proteins (IAPs) and anticancer activity.
PDB None

Name CHEMBL481422
Affinity Ki = 8.2uM
Assay description Binding affinity to BIR2 domain of XIAP by fluorescence polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22148838
Doc title Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents.
PDB None

Name CHEMBL481422
Affinity IC50 = 1240nM
Assay description Binding affinity to BIR2-BIR3 domain of XIAP by fluorescence polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22148838
Doc title Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents.
PDB None

Name CHEMBL481422
Affinity Ki = 26nM
Assay description Displacement of fluorescent SM5F peptide from His-tagged human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/19138149
Doc title Design, synthesis, and evaluation of potent, nonpeptidic mimetics of second mitochondria-derived activator of caspases.
PDB None

Name CHEMBL481422
Affinity Ki = 408nM
Assay description Binding affinity to human XIAP linker BIR2-BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21462933
Doc title Potent bivalent Smac mimetics: effect of the linker on binding to inhibitor of apoptosis proteins (IAPs) and anticancer activity.
PDB None

Name CHEMBL481422
Affinity IC50 = 18.9uM
Assay description Binding affinity to BIR2 domain of XIAP by fluorescence polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22148838
Doc title Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents.
PDB None

Name CHEMBL481422
Affinity Ki = 191nM
Assay description Binding affinity to BIR3 domain of XIAP by fluorescence polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22148838
Doc title Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents.
PDB None

Name CHEMBL481422
Affinity IC50 = 635.7nM
Assay description Displacement of fluorescent SM5F peptide from His-tagged human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20684551
Doc title Nonpeptidic and potent small-molecule inhibitors of cIAP-1/2 and XIAP proteins.
PDB None

Name CHEMBL481422
Affinity IC50 = 636nM
Assay description Binding affinity to BIR3 domain of XIAP by fluorescence polarization assay
-- Homologous single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22148838
Doc title Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents.
PDB None

Name CHEMBL481422
Affinity Ki = 190.7nM
Assay description Displacement of fluorescent SM5F peptide from His-tagged human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/20684551
Doc title Nonpeptidic and potent small-molecule inhibitors of cIAP-1/2 and XIAP proteins.
PDB None

Name CHEMBL481422
Affinity Ki = 248nM
Assay description Binding affinity to His-tagged human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) after 2 to 3 hrs by fluorescence polarization-based assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21462933
Doc title Potent bivalent Smac mimetics: effect of the linker on binding to inhibitor of apoptosis proteins (IAPs) and anticancer activity.
PDB None

Name CHEMBL485721
Affinity Ki = 0.014uM
Assay description Binding affinity to N-terminal 6xHis-tagged human cloned XIAP BIR3 domain expressed in Escherichia coli BL21 (DE3) by fluorescence polarization-based competitive binding assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18954041
Doc title Structure-based design, synthesis, evaluation, and crystallographic studies of conformationally constrained Smac mimetics as inhibitors of the X-linked inhibitor of apoptosis protein (XIAP).
PDB None

Name CHEMBL486330
Affinity Ki = 12.97uM
Assay description Binding affinity to N-terminal 6xHis-tagged human cloned XIAP BIR3 domain expressed in Escherichia coli BL21 (DE3) by fluorescence polarization-based competitive binding assay
-- Direct single protein target assigned: XIAP_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/18954041
Doc title Structure-based design, synthesis, evaluation, and crystallographic studies of conformationally constrained Smac mimetics as inhibitors of the X-linked inhibitor of apoptosis protein (XIAP).
PDB None