BRDT

Bromodomain testis-specific protein

Reviewed UniProt entries for BRDT and its protein partners


UniProt code UniProt Name Protein Name Gene Name Organism Length
F1QW93 BRDT_DANRE Bromodomain testis-specific protein brdt si:dkeyp-85h7.3 Danio rerio (Zebrafish) (Brachydanio rerio) 918
Q58F21 BRDT_HUMAN Bromodomain testis-specific protein (Cancer/testis antigen 9) (CT9) (RING3-like protein) BRDT Homo sapiens (Human) 947
Q4R8Y1 BRDT_MACFA Bromodomain testis-specific protein BRDT QtsA-11165 Macaca fascicularis (Crab-eating macaque) (Cynomolgus monkey) 947
Q91Y44 BRDT_MOUSE Bromodomain testis-specific protein (Bromodomain-containing female sterile homeotic-like protein) (RING3-like protein) Brdt Fsrg3 Mus musculus (Mouse) 956
D4A7T3 BRDT_RAT Bromodomain testis-specific protein Brdt Rattus norvegicus (Rat) 952
F7DRV9 BRDT_XENTR Bromodomain testis-specific protein brdt Xenopus tropicalis (Western clawed frog) (Silurana tropicalis) 933

Small molecules tested in BRDT binding assays:

30 datapoints for 29 distinct small molecules


Name Jq1
Affinity KD = 44-190 nM
Assay description ITC
-- Direct single protein target assigned: BRDT_HUMAN (Expert curation) --
DOI http://www.cell.com/retrieve/pii/S0092867412009294
Doc title Small-Molecule Inhibition of BRDT for Male Contraception
PDB 4FLP - (JQ1)

Name CHEMBL1201169
Affinity Not Active
Assay description Binding affinity to BRDT-BD1 assessed as change in melting temperature at 10 uM by protein stability shift assay
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22137933
Doc title Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
PDB None

Name CHEMBL1828978
Affinity deltaTm = 3.2degrees C
Assay description Binding affinity to BRDT assessed as change in melting temperature at 100 uM by differential scanning fluorimetry
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21851057
Doc title 3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.
PDB None

Name CHEMBL1828979
Affinity deltaTm = 0degrees C
Assay description Binding affinity to BRDT assessed as change in melting temperature at 100 uM by differential scanning fluorimetry
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21851057
Doc title 3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.
PDB None

Name CHEMBL1828980
Affinity deltaTm = -0.2degrees C
Assay description Binding affinity to BRDT assessed as change in melting temperature at 100 uM by differential scanning fluorimetry
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21851057
Doc title 3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.
PDB None

Name CHEMBL1828981
Affinity deltaTm = -0.4degrees C
Assay description Binding affinity to BRDT assessed as change in melting temperature at 100 uM by differential scanning fluorimetry
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21851057
Doc title 3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.
PDB None

Name CHEMBL1828982
Affinity deltaTm = 1.6degrees C
Assay description Binding affinity to BRDT assessed as change in melting temperature at 100 uM by differential scanning fluorimetry
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21851057
Doc title 3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.
PDB None

Name CHEMBL1828983
Affinity deltaTm = 1.1degrees C
Assay description Binding affinity to BRDT assessed as change in melting temperature at 100 uM by differential scanning fluorimetry
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21851057
Doc title 3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.
PDB None

Name CHEMBL1828984
Affinity deltaTm = -0.8degrees C
Assay description Binding affinity to BRDT assessed as change in melting temperature at 100 uM by differential scanning fluorimetry
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21851057
Doc title 3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.
PDB None

Name CHEMBL1828985
Affinity deltaTm = 0.2degrees C
Assay description Binding affinity to BRDT assessed as change in melting temperature at 100 uM by differential scanning fluorimetry
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21851057
Doc title 3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.
PDB None

Name CHEMBL1828986
Affinity deltaTm = 3.5degrees C
Assay description Binding affinity to BRDT assessed as change in melting temperature at 100 uM by differential scanning fluorimetry
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/21851057
Doc title 3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.
PDB None

Name CHEMBL1957266
Affinity Kd = 190.1nM
Assay description Binding affinity to BRDT-BD1 by isothermal titration calorimetry
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22316554
Doc title Development of live-cell imaging probes for monitoring histone modifications.
PDB None

Name CHEMBL1958335
Affinity deltaTm <= 2degrees C
Assay description Binding affinity to BRDT-BD1 assessed as change in melting temperature at 100 uM by protein stability shift assay
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22137933
Doc title Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
PDB None

Name CHEMBL1958336
Affinity deltaTm <= 2degrees C
Assay description Binding affinity to BRDT-BD1 assessed as change in melting temperature at 100 uM by protein stability shift assay
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22137933
Doc title Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
PDB None

Name CHEMBL1958337
Affinity deltaTm <= 2degrees C
Assay description Binding affinity to BRDT-BD1 assessed as change in melting temperature at 100 uM by protein stability shift assay
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22137933
Doc title Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
PDB None

Name CHEMBL1958337
Affinity Active
Assay description Binding affinity to BRDT-BD1 assessed as change in melting temperature at 10 uM by protein stability shift assay
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22137933
Doc title Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
PDB None

Name CHEMBL1958338
Affinity deltaTm <= 2degrees C
Assay description Binding affinity to BRDT-BD1 assessed as change in melting temperature at 100 uM by protein stability shift assay
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22137933
Doc title Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
PDB None

Name CHEMBL1958339
Affinity deltaTm <= 2degrees C
Assay description Binding affinity to BRDT-BD1 assessed as change in melting temperature at 100 uM by protein stability shift assay
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22137933
Doc title Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
PDB None

Name CHEMBL1958340
Affinity deltaTm <= 2degrees C
Assay description Binding affinity to BRDT-BD1 assessed as change in melting temperature at 100 uM by protein stability shift assay
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22137933
Doc title Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
PDB None

Name CHEMBL1958341
Affinity deltaTm <= 2degrees C
Assay description Binding affinity to BRDT-BD1 assessed as change in melting temperature at 100 uM by protein stability shift assay
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22137933
Doc title Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
PDB None

Name CHEMBL1958342
Affinity deltaTm <= 2degrees C
Assay description Binding affinity to BRDT-BD1 assessed as change in melting temperature at 100 uM by protein stability shift assay
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22137933
Doc title Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
PDB None

Name CHEMBL1958343
Affinity deltaTm <= 2degrees C
Assay description Binding affinity to BRDT-BD1 assessed as change in melting temperature at 100 uM by protein stability shift assay
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22137933
Doc title Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
PDB None

Name CHEMBL1958344
Affinity deltaTm <= 2degrees C
Assay description Binding affinity to BRDT-BD1 assessed as change in melting temperature at 100 uM by protein stability shift assay
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22137933
Doc title Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
PDB None

Name CHEMBL1958345
Affinity deltaTm <= 2degrees C
Assay description Binding affinity to BRDT-BD1 assessed as change in melting temperature at 100 uM by protein stability shift assay
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22137933
Doc title Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
PDB None

Name CHEMBL1958346
Affinity deltaTm <= 2degrees C
Assay description Binding affinity to BRDT-BD1 assessed as change in melting temperature at 100 uM by protein stability shift assay
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22137933
Doc title Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
PDB None

Name CHEMBL2179387
Affinity deltaTm = 2.08degrees C
Assay description Binding affinity to BRDT isoform 1 assessed as change in melting temperature at 10 uM by thermal shift assay
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/23095041
Doc title Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.
PDB None

Name CHEMBL52030
Affinity Not Active
Assay description Binding affinity to BRDT-BD1 assessed as change in melting temperature at 10 uM by protein stability shift assay
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22137933
Doc title Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
PDB None

Name CHEMBL646
Affinity Active
Assay description Binding affinity to BRDT-BD1 assessed as change in melting temperature at 10 uM by protein stability shift assay
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22137933
Doc title Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
PDB None

Name CHEMBL655
Affinity Active
Assay description Binding affinity to BRDT-BD1 assessed as change in melting temperature at 10 uM by protein stability shift assay
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22137933
Doc title Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
PDB None

Name CHEMBL661
Affinity Active
Assay description Binding affinity to BRDT-BD1 assessed as change in melting temperature at 10 uM by protein stability shift assay
-- Homologous single protein target assigned: BRDT_HUMAN (Autocuration) --
DOI http://www.ncbi.nlm.nih.gov/pubmed/22137933
Doc title Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
PDB None

5 PDB entries for BRDT and its protein partners


2RFJ
Histone recognition and large-scale structural analysis of the human bromodomain family.

Entity type Code Description
polypeptide(L) Q58F21 Bromodomain testis-specific protein

2WP1
Cooperative Binding of Two Acetylation Marks on a Histone Tail by a Single Bromodomain.

Entity type Code Description
polypeptide(L) Q91Y44 BROMODOMAIN TESTIS-SPECIFIC PROTEIN
polypeptide(L) B9EI85 HISTONE H3

2WP2
Cooperative Binding of Two Acetylation Marks on a Histone Tail by a Single Bromodomain.

Entity type Code Description
polypeptide(L) Q91Y44 BROMODOMAIN TESTIS-SPECIFIC PROTEIN
polypeptide(L) P62806 HISTONE H4

4FLP
Small-Molecule Inhibition of BRDT for Male Contraception.

Entity type Code Description
polypeptide(L) Q58F21 Bromodomain testis-specific protein
Ligand JQ1 (6S)-6-(2-TERT-BUTOXY-2-OXOETHYL)-4-(4-CHLOROPHENYL)-2,3,9-TRIMETHYL-6,7-DIHYDROTHIENO[3,2-F][1,2,4]TRIAZOLO[4,3-A][1,4]DIAZEPIN-10-IUM

4KCX
The cyclin-dependent kinase inhibitor dinaciclib interacts with the acetyl-lysine recognition site of bromodomains.

Entity type Code Description
polypeptide(L) Q58F21 Bromodomain testis-specific protein
Ligand 1QK 3-[({3-ETHYL-5-[(2S)-2-(2-HYDROXYETHYL)PIPERIDIN-1-YL]PYRAZOLO[1,5-A]PYRIMIDIN-7-YL}AMINO)METHYL]-1-HYDROXYPYRIDINIUM