STAT3

Signal transducer and activator of transcription 3

Reviewed UniProt entries for STAT3 and its protein partners


UniProt code UniProt Name Protein Name Gene Name Organism Length
Q9PVX8 STA31_XENLA Signal transducer and activator of transcription 3.1 (Protein Stat3) (Xstat3) stat3.1 stat3 Xenopus laevis (African clawed frog) 769
Q7ZXK3 STA32_XENLA Signal transducer and activator of transcription 3.2 (Protein Stat3-A) stat3.2 stat3-a Xenopus laevis (African clawed frog) 766
P61635 STAT3_BOVIN Signal transducer and activator of transcription 3 STAT3 Bos taurus (Bovine) 770
Q6DV79 STAT3_CHICK Signal transducer and activator of transcription 3 STAT3 RCJMB04_38l20 Gallus gallus (Chicken) 771
P40763 STAT3_HUMAN Signal transducer and activator of transcription 3 (Acute-phase response factor) STAT3 APRF Homo sapiens (Human) 770
P42227 STAT3_MOUSE Signal transducer and activator of transcription 3 (Acute-phase response factor) Stat3 Aprf Mus musculus (Mouse) 770
Q19S50 STAT3_PIG Signal transducer and activator of transcription 3 STAT3 Sus scrofa (Pig) 770
P52631 STAT3_RAT Signal transducer and activator of transcription 3 Stat3 Rattus norvegicus (Rat) 770

Small molecules tested in STAT3 binding assays:

72 datapoints for 59 distinct small molecules


Name CHEMBL156046
Affinity IC50 = 4uM
Assay description Inhibition of Stat3 (Signal transduction and activator of transcription 3) dimerization measured by EMSAs (Electrophoretic mobility shift assay)
-- Homologous single protein target assigned: STAT3_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12639546
Doc title Identification of a high-affinity phosphopeptide inhibitor of Stat3.
PDB None

Name CHEMBL156448
Affinity IC50 = 8uM
Assay description Inhibition of Stat3 (Signal transduction and activator of transcription 3) dimerization measured by EMSAs (Electrophoretic mobility shift assay)
-- Homologous single protein target assigned: STAT3_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12639546
Doc title Identification of a high-affinity phosphopeptide inhibitor of Stat3.
PDB None

Name CHEMBL160353
Affinity IC50 = 0.6uM
Assay description Inhibition of Stat3 (Signal transduction and activator of transcription 3) dimerization measured by EMSAs (Electrophoretic mobility shift assay)
-- Homologous single protein target assigned: STAT3_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12639546
Doc title Identification of a high-affinity phosphopeptide inhibitor of Stat3.
PDB None

Name CHEMBL160658
Affinity IC50 = 1uM
Assay description Inhibition of Stat3 (Signal transduction and activator of transcription 3) dimerization measured by EMSAs (Electrophoretic mobility shift assay)
-- Homologous single protein target assigned: STAT3_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12639546
Doc title Identification of a high-affinity phosphopeptide inhibitor of Stat3.
PDB None

Name CHEMBL1681824
Affinity INH = 50%
Assay description Inhibition of STAT3 dimerization in v-Src transformed mouse NIH3T3 cells assessed as suppression of STAT3-DNA binding activity in nucleus at 100 uM after 6 hrs by electrophoretic mobility shift assay
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21216604
Doc title Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
PDB None

Name CHEMBL1681824
Affinity IC50 = 5uM
Assay description Inhibition of STAT3 dimerization in mouse NIH3T3 cells expressing v-Src assessed as disruption of STAT3-STAT3: DNA complexation in nucleus after 30 mins by electrophoretic mobility shift assay
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21216604
Doc title Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
PDB None

Name CHEMBL1681824
Affinity Active
Assay description Inhibition of STAT3 dimerization in v-Src transformed mouse NIH3T3 cells assessed as suppression of STAT3-DNA binding activity in nucleus at 100 uM after 24 hrs by electrophoretic mobility shift assay
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21216604
Doc title Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
PDB None

Name CHEMBL1681825
Affinity IC50 = 60uM
Assay description Inhibition of STAT3 dimerization in mouse NIH3T3 cells expressing v-Src assessed as disruption of STAT3-STAT3: DNA complexation in nucleus after 30 mins by electrophoretic mobility shift assay
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21216604
Doc title Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
PDB None

Name CHEMBL1681826
Affinity IC50 = 112uM
Assay description Inhibition of STAT3 dimerization in mouse NIH3T3 cells expressing v-Src assessed as disruption of STAT3-STAT3: DNA complexation in nucleus after 30 mins by electrophoretic mobility shift assay
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21216604
Doc title Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
PDB None

Name CHEMBL1681827
Affinity IC50 = 188uM
Assay description Inhibition of STAT3 dimerization in mouse NIH3T3 cells expressing v-Src assessed as disruption of STAT3-STAT3: DNA complexation in nucleus after 30 mins by electrophoretic mobility shift assay
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21216604
Doc title Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
PDB None

Name CHEMBL1681828
Affinity IC50 = 92uM
Assay description Inhibition of STAT3 dimerization in mouse NIH3T3 cells expressing v-Src assessed as disruption of STAT3-STAT3: DNA complexation in nucleus after 30 mins by electrophoretic mobility shift assay
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21216604
Doc title Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
PDB None

Name CHEMBL1681829
Affinity IC50 = 66uM
Assay description Inhibition of STAT3 dimerization in mouse NIH3T3 cells expressing v-Src assessed as disruption of STAT3-STAT3: DNA complexation in nucleus after 30 mins by electrophoretic mobility shift assay
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21216604
Doc title Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
PDB None

Name CHEMBL1684872
Affinity Active
Assay description Inhibition of STAT3 dimerization in v-Src transformed mouse NIH3T3 cells assessed as suppression of STAT3-DNA binding activity in nucleus at 100 uM after 24 hrs by electrophoretic mobility shift assay
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21216604
Doc title Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
PDB None

Name CHEMBL1684872
Affinity INH > 80%
Assay description Inhibition of STAT3 dimerization in v-Src transformed mouse NIH3T3 cells assessed as suppression of STAT3-DNA binding activity in nucleus at 100 uM after 6 hrs by electrophoretic mobility shift assay
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21216604
Doc title Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
PDB None

Name CHEMBL1684872
Affinity IC50 = 73.1uM
Assay description Inhibition of STAT3 dimerization in mouse NIH3T3 cells expressing v-Src assessed as disruption of STAT3-STAT3: DNA complexation in nucleus after 30 mins by electrophoretic mobility shift assay
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21216604
Doc title Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
PDB None

Name CHEMBL1684873
Affinity IC50 = 33uM
Assay description Inhibition of STAT3 dimerization in mouse NIH3T3 cells expressing v-Src assessed as disruption of STAT3-STAT3: DNA complexation in nucleus after 30 mins by electrophoretic mobility shift assay
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21216604
Doc title Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
PDB None

Name CHEMBL1684874
Affinity IC50 > 200uM
Assay description Inhibition of STAT3 dimerization in mouse NIH3T3 cells expressing v-Src assessed as disruption of STAT3-STAT3: DNA complexation in nucleus after 30 mins by electrophoretic mobility shift assay
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21216604
Doc title Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
PDB None

Name CHEMBL1684875
Affinity Active
Assay description Inhibition of STAT3 dimerization in v-Src transformed mouse NIH3T3 cells assessed as suppression of STAT3-DNA binding activity in nucleus at 100 uM after 24 hrs by electrophoretic mobility shift assay
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21216604
Doc title Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
PDB None

Name CHEMBL1684875
Affinity IC50 = 103uM
Assay description Inhibition of STAT3 dimerization in mouse NIH3T3 cells expressing v-Src assessed as disruption of STAT3-STAT3: DNA complexation in nucleus after 30 mins by electrophoretic mobility shift assay
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21216604
Doc title Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
PDB None

Name CHEMBL1684875
Affinity Active
Assay description Inhibition of STAT3 dimerization in v-Src transformed mouse NIH3T3 cells assessed as suppression of STAT3-DNA binding activity in nucleus at 100 uM after 6 hrs by electrophoretic mobility shift assay
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21216604
Doc title Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
PDB None

Name CHEMBL1684876
Affinity Not Active
Assay description Inhibition of STAT3 dimerization in v-Src transformed mouse NIH3T3 cells assessed as suppression of STAT3-DNA binding activity in nucleus at 100 uM after 24 hrs by electrophoretic mobility shift assay
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21216604
Doc title Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
PDB None

Name CHEMBL1684876
Affinity IC50 = 190uM
Assay description Inhibition of STAT3 dimerization in mouse NIH3T3 cells expressing v-Src assessed as disruption of STAT3-STAT3: DNA complexation in nucleus after 30 mins by electrophoretic mobility shift assay
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21216604
Doc title Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
PDB None

Name CHEMBL1684876
Affinity Not Active
Assay description Inhibition of STAT3 dimerization in v-Src transformed mouse NIH3T3 cells assessed as suppression of STAT3-DNA binding activity in nucleus at 100 uM after 6 hrs by electrophoretic mobility shift assay
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21216604
Doc title Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
PDB None

Name CHEMBL1684877
Affinity IC50 = 62uM
Assay description Inhibition of STAT3 dimerization in mouse NIH3T3 cells expressing v-Src assessed as disruption of STAT3-STAT3: DNA complexation in nucleus after 30 mins by electrophoretic mobility shift assay
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21216604
Doc title Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
PDB None

Name CHEMBL1684878
Affinity IC50 = 64uM
Assay description Inhibition of STAT3 dimerization in mouse NIH3T3 cells expressing v-Src assessed as disruption of STAT3-STAT3: DNA complexation in nucleus after 30 mins by electrophoretic mobility shift assay
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21216604
Doc title Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
PDB None

Name CHEMBL1684879
Affinity IC50 = 40uM
Assay description Inhibition of STAT3 dimerization in mouse NIH3T3 cells expressing v-Src assessed as disruption of STAT3-STAT3: DNA complexation in nucleus after 30 mins by electrophoretic mobility shift assay
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21216604
Doc title Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
PDB None

Name CHEMBL1829786
Affinity IC50 = 35uM
Assay description Inhibition of STAT3 dimerization in v-Src transformed mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT3-DNA interaction in nucleus after 30 mins by EMSA
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22650325
Doc title Small molecule inhibitors of signal transducer and activator of transcription 3 (Stat3) protein.
PDB None

Name CHEMBL2023986
Affinity IC50 = 43uM
Assay description Inhibition of STAT3 dimerization in v-Src transformed mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT3-DNA interaction in nucleus after 30 mins by EMSA
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22650325
Doc title Small molecule inhibitors of signal transducer and activator of transcription 3 (Stat3) protein.
PDB None

Name CHEMBL2023987
Affinity IC50 = 50uM
Assay description Inhibition of STAT3 dimerization in v-Src transformed mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT3-DNA interaction in nucleus after 30 mins by EMSA
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22650325
Doc title Small molecule inhibitors of signal transducer and activator of transcription 3 (Stat3) protein.
PDB None

Name CHEMBL2171897
Affinity IC50 = 25uM
Assay description Inhibition of STAT3 dimerization in v-Src transformed mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT3-DNA interaction in nucleus after 30 mins by EMSA
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22650325
Doc title Small molecule inhibitors of signal transducer and activator of transcription 3 (Stat3) protein.
PDB None

Name CHEMBL2172013
Affinity IC50 = 43uM
Assay description Inhibition of STAT3 dimerization in v-Src transformed mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT3-DNA interaction in nucleus after 30 mins by EMSA
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22650325
Doc title Small molecule inhibitors of signal transducer and activator of transcription 3 (Stat3) protein.
PDB None

Name CHEMBL2172014
Affinity IC50 = 45uM
Assay description Inhibition of STAT3 dimerization in v-Src transformed mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT3-DNA interaction in nucleus after 30 mins by EMSA
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22650325
Doc title Small molecule inhibitors of signal transducer and activator of transcription 3 (Stat3) protein.
PDB None

Name CHEMBL2172015
Affinity IC50 = 33uM
Assay description Inhibition of STAT3 dimerization in v-Src transformed mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT3-DNA interaction in nucleus after 30 mins by EMSA
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22650325
Doc title Small molecule inhibitors of signal transducer and activator of transcription 3 (Stat3) protein.
PDB None

Name CHEMBL2172016
Affinity IC50 = 90uM
Assay description Inhibition of STAT3 dimerization in v-Src transformed mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT3-DNA interaction in nucleus after 30 mins by EMSA
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22650325
Doc title Small molecule inhibitors of signal transducer and activator of transcription 3 (Stat3) protein.
PDB None

Name CHEMBL2172017
Affinity IC50 = 28uM
Assay description Inhibition of STAT3 dimerization in v-Src transformed mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT3-DNA interaction in nucleus after 30 mins by EMSA
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22650325
Doc title Small molecule inhibitors of signal transducer and activator of transcription 3 (Stat3) protein.
PDB None

Name CHEMBL2172018
Affinity IC50 = 58uM
Assay description Inhibition of STAT3 dimerization in v-Src transformed mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT3-DNA interaction in nucleus after 30 mins by EMSA
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22650325
Doc title Small molecule inhibitors of signal transducer and activator of transcription 3 (Stat3) protein.
PDB None

Name CHEMBL232998
Affinity Not Active
Assay description Inhibition of STAT3 dimer DNA binding activity after 30 mins
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17336521
Doc title Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains.
PDB None

Name CHEMBL234465
Affinity IC50 = 74uM
Assay description Inhibition of STAT3 dimer DNA binding activity after 30 mins
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17336521
Doc title Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains.
PDB None

Name CHEMBL234465
Affinity IC50 = 58uM
Assay description Inhibition of STAT3 dimer DNA binding activity after 30 mins
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17336521
Doc title Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains.
PDB None

Name CHEMBL234466
Affinity IC50 = 620uM
Assay description Inhibition of STAT3 dimer DNA binding activity after 30 mins
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17336521
Doc title Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains.
PDB None

Name CHEMBL234817
Affinity IC50 = 123uM
Assay description Inhibition of STAT3 dimer DNA binding activity after 30 mins
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17336521
Doc title Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains.
PDB None

Name CHEMBL2414121
Affinity INH = 40.9%
Assay description Binding affinity to STAT3 SH2 domain (unknown origin) using 5-FAM-SpYLPQTV as probe assessed as inhibition of protein dimerization at 500 uM after 60 mins by fluorescence polarization assay relative to control
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23791367
Doc title Anticancer activity and SAR studies of substituted 1,4-naphthoquinones.
PDB None

Name CHEMBL2414122
Affinity INH = 22.2%
Assay description Binding affinity to STAT3 SH2 domain (unknown origin) using 5-FAM-SpYLPQTV as probe assessed as inhibition of protein dimerization at 500 uM after 60 mins by fluorescence polarization assay relative to control
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23791367
Doc title Anticancer activity and SAR studies of substituted 1,4-naphthoquinones.
PDB None

Name CHEMBL2414123
Affinity INH = 77%
Assay description Binding affinity to STAT3 SH2 domain (unknown origin) using 5-FAM-SpYLPQTV as probe assessed as inhibition of protein dimerization at 500 uM after 60 mins by fluorescence polarization assay relative to control
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23791367
Doc title Anticancer activity and SAR studies of substituted 1,4-naphthoquinones.
PDB None

Name CHEMBL2414123
Affinity Ki = 18.2uM
Assay description Binding affinity to STAT3 SH2 domain (unknown origin) using 5-FAM-SpYLPQTV as probe assessed as inhibition of protein dimerization after 60 mins by fluorescence polarization assay
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23791367
Doc title Anticancer activity and SAR studies of substituted 1,4-naphthoquinones.
PDB None

Name CHEMBL2414128
Affinity INH = 11.4%
Assay description Binding affinity to STAT3 SH2 domain (unknown origin) using 5-FAM-SpYLPQTV as probe assessed as inhibition of protein dimerization at 500 uM after 60 mins by fluorescence polarization assay relative to control
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23791367
Doc title Anticancer activity and SAR studies of substituted 1,4-naphthoquinones.
PDB None

Name CHEMBL2414129
Affinity INH = -2.5%
Assay description Binding affinity to STAT3 SH2 domain (unknown origin) using 5-FAM-SpYLPQTV as probe assessed as inhibition of protein dimerization at 500 uM after 60 mins by fluorescence polarization assay relative to control
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23791367
Doc title Anticancer activity and SAR studies of substituted 1,4-naphthoquinones.
PDB None

Name CHEMBL2414131
Affinity INH = 14.3%
Assay description Binding affinity to STAT3 SH2 domain (unknown origin) using 5-FAM-SpYLPQTV as probe assessed as inhibition of protein dimerization at 500 uM after 60 mins by fluorescence polarization assay relative to control
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23791367
Doc title Anticancer activity and SAR studies of substituted 1,4-naphthoquinones.
PDB None

Name CHEMBL2414132
Affinity INH = 74.4%
Assay description Binding affinity to STAT3 SH2 domain (unknown origin) using 5-FAM-SpYLPQTV as probe assessed as inhibition of protein dimerization at 500 uM after 60 mins by fluorescence polarization assay relative to control
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23791367
Doc title Anticancer activity and SAR studies of substituted 1,4-naphthoquinones.
PDB None

Name CHEMBL2414132
Affinity Ki = 13.3uM
Assay description Binding affinity to STAT3 SH2 domain (unknown origin) using 5-FAM-SpYLPQTV as probe assessed as inhibition of protein dimerization after 60 mins by fluorescence polarization assay
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23791367
Doc title Anticancer activity and SAR studies of substituted 1,4-naphthoquinones.
PDB None

Name CHEMBL2414133
Affinity INH = 57.9%
Assay description Binding affinity to STAT3 SH2 domain (unknown origin) using 5-FAM-SpYLPQTV as probe assessed as inhibition of protein dimerization at 500 uM after 60 mins by fluorescence polarization assay relative to control
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23791367
Doc title Anticancer activity and SAR studies of substituted 1,4-naphthoquinones.
PDB None

Name CHEMBL2414134
Affinity INH = 67.5%
Assay description Binding affinity to STAT3 SH2 domain (unknown origin) using 5-FAM-SpYLPQTV as probe assessed as inhibition of protein dimerization at 500 uM after 60 mins by fluorescence polarization assay relative to control
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23791367
Doc title Anticancer activity and SAR studies of substituted 1,4-naphthoquinones.
PDB None

Name CHEMBL2414136
Affinity INH = 33.7%
Assay description Binding affinity to STAT3 SH2 domain (unknown origin) using 5-FAM-SpYLPQTV as probe assessed as inhibition of protein dimerization at 500 uM after 60 mins by fluorescence polarization assay relative to control
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23791367
Doc title Anticancer activity and SAR studies of substituted 1,4-naphthoquinones.
PDB None

Name CHEMBL2414137
Affinity INH = 47.6%
Assay description Binding affinity to STAT3 SH2 domain (unknown origin) using 5-FAM-SpYLPQTV as probe assessed as inhibition of protein dimerization at 500 uM after 60 mins by fluorescence polarization assay relative to control
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23791367
Doc title Anticancer activity and SAR studies of substituted 1,4-naphthoquinones.
PDB None

Name CHEMBL2414138
Affinity INH = 44.7%
Assay description Binding affinity to STAT3 SH2 domain (unknown origin) using 5-FAM-SpYLPQTV as probe assessed as inhibition of protein dimerization at 500 uM after 60 mins by fluorescence polarization assay relative to control
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23791367
Doc title Anticancer activity and SAR studies of substituted 1,4-naphthoquinones.
PDB None

Name CHEMBL295316
Affinity INH = 58.1%
Assay description Binding affinity to STAT3 SH2 domain (unknown origin) using 5-FAM-SpYLPQTV as probe assessed as inhibition of protein dimerization at 500 uM after 60 mins by fluorescence polarization assay relative to control
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23791367
Doc title Anticancer activity and SAR studies of substituted 1,4-naphthoquinones.
PDB None

Name CHEMBL346706
Affinity IC50 > 150uM
Assay description Inhibition of Stat3 (Signal transduction and activator of transcription 3) dimerization measured by EMSAs (Electrophoretic mobility shift assay)
-- Homologous single protein target assigned: STAT3_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12639546
Doc title Identification of a high-affinity phosphopeptide inhibitor of Stat3.
PDB None

Name CHEMBL348612
Affinity IC50 = 80uM
Assay description Inhibition of Stat3 (Signal transduction and activator of transcription 3) dimerization measured by EMSAs (Electrophoretic mobility shift assay)
-- Homologous single protein target assigned: STAT3_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12639546
Doc title Identification of a high-affinity phosphopeptide inhibitor of Stat3.
PDB None

Name CHEMBL348880
Affinity IC50 > 6uM
Assay description Inhibition of Stat3 (Signal transduction and activator of transcription 3) dimerization measured by EMSAs (Electrophoretic mobility shift assay)
-- Homologous single protein target assigned: STAT3_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12639546
Doc title Identification of a high-affinity phosphopeptide inhibitor of Stat3.
PDB None

Name CHEMBL351757
Affinity IC50 = 1.5uM
Assay description Inhibition of Stat3 (Signal transduction and activator of transcription 3) dimerization measured by EMSAs (Electrophoretic mobility shift assay)
-- Homologous single protein target assigned: STAT3_HUMAN (Expert curation) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/12639546
Doc title Identification of a high-affinity phosphopeptide inhibitor of Stat3.
PDB None

Name CHEMBL392556
Affinity IC50 = 42uM
Assay description Inhibition of STAT3 dimerization in v-Src transformed mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT3-DNA interaction in nucleus after 30 mins by EMSA
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22650325
Doc title Small molecule inhibitors of signal transducer and activator of transcription 3 (Stat3) protein.
PDB None

Name CHEMBL392556
Affinity IC50 = 310uM
Assay description Inhibition of STAT3 dimer DNA binding activity after 30 mins
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17336521
Doc title Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains.
PDB None

Name CHEMBL393817
Affinity IC50 = 58uM
Assay description Inhibition of STAT3 dimer DNA binding activity after 30 mins
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17336521
Doc title Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains.
PDB None

Name CHEMBL398067
Affinity IC50 = 800uM
Assay description Inhibition of STAT3 dimer DNA binding activity after 30 mins
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17336521
Doc title Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains.
PDB None

Name CHEMBL412549
Affinity IC50 = 31uM
Assay description Inhibition of STAT3 dimer DNA binding activity after 30 mins
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17336521
Doc title Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains.
PDB None

Name CHEMBL412781
Affinity Not Active
Assay description Inhibition of STAT3 dimer DNA binding activity after 30 mins
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17336521
Doc title Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains.
PDB None

Name CHEMBL412782
Affinity Not Active
Assay description Inhibition of STAT3 dimer DNA binding activity after 30 mins
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17336521
Doc title Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains.
PDB None

Name CHEMBL43612
Affinity INH = 76.4%
Assay description Binding affinity to STAT3 SH2 domain (unknown origin) using 5-FAM-SpYLPQTV as probe assessed as inhibition of protein dimerization at 500 uM after 60 mins by fluorescence polarization assay relative to control
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23791367
Doc title Anticancer activity and SAR studies of substituted 1,4-naphthoquinones.
PDB None

Name CHEMBL438852
Affinity IC50 = 310uM
Assay description Inhibition of STAT3 dimer DNA binding activity after 30 mins
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/17336521
Doc title Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains.
PDB None

Name CHEMBL477936
Affinity IC50 = 86uM
Assay description Inhibition of STAT3 dimerization in v-Src transformed mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT3-DNA interaction in nucleus after 30 mins by EMSA
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22650325
Doc title Small molecule inhibitors of signal transducer and activator of transcription 3 (Stat3) protein.
PDB None

Name CHEMBL477936
Affinity IC50 = 86uM
Assay description Inhibition of STAT3 dimerization in EGF-stimulated mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT3-DNA interaction after 30 mins by EMSA
-- Direct single protein target assigned: STAT3_MOUSE (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22650325
Doc title Small molecule inhibitors of signal transducer and activator of transcription 3 (Stat3) protein.
PDB None

Name CHEMBL92659
Affinity INH = 43%
Assay description Binding affinity to STAT3 SH2 domain (unknown origin) using 5-FAM-SpYLPQTV as probe assessed as inhibition of protein dimerization at 500 uM after 60 mins by fluorescence polarization assay relative to control
-- Direct single protein target assigned: STAT3_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23791367
Doc title Anticancer activity and SAR studies of substituted 1,4-naphthoquinones.
PDB None

3 PDB entries for STAT3 and its protein partners


1BG1
Three-dimensional structure of the Stat3beta homodimer bound to DNA.

Entity type Code Description
polydeoxyribonucleotide 1BG1 DNA (5'-D(*TP*GP*CP*AP*TP*TP*TP*CP*CP*CP*GP*TP*AP*AP*AP*TP*CP*T)-3')
polypeptide(L) P42227 PROTEIN (TRANSCRIPTION FACTOR STAT3B)

3CWG
Crystal structure of unphosphorylated STAT3 core fragment.

Entity type Code Description
polypeptide(L) P42227 Signal transducer and activator of transcription 3

4E68
Observation of unphosphorylated STAT3 core protein binding to target dsDNA by PEMSA and X-ray crystallography.

Entity type Code Description
polydeoxyribonucleotide 4E68 DNA (5'-D(*TP*GP*CP*AP*TP*TP*TP*CP*CP*CP*GP*TP*AP*AP*AP*TP*CP*T)-3')
polypeptide(L) P42227 Signal transducer and activator of transcription 3