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Target
Bromodomain-containing protein 3
Ligand
BDBM50441168
Substrate
n/a
Meas. Tech.
ChEMBL_985089 (CHEMBL2433594)
IC50
1000±n/a nM
Citation
 Mirguet, O; Gosmini, R; Toum, J; Clément, CA; Barnathan, M; Brusq, JM; Mordaunt, JE; Grimes, RM; Crowe, M; Pineau, O; Ajakane, M; Daugan, A; Jeffrey, P; Cutler, L; Haynes, AC; Smithers, NN; Chung, CW; Bamborough, P; Uings, IJ; Lewis, A; Witherington, J; Parr, N; Prinjha, RK; Nicodème, E Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains. J Med Chem 56:7501-15 (2013) [PubMed]  Article 
Target
Name:
Bromodomain-containing protein 3
Synonyms:
BRD3 | BRD3_HUMAN | Bromodomain and extra-terminal motif (BET) | Bromodomain-containing protein 3 | Bromodomain-containing protein 3 (BRD3) | KIAA0043 | RING3-like protein | RING3L
Type:
Protein
Mol. Mass.:
79571.81
Organism:
Homo sapiens (Human)
Description:
Q15059
Residue:
726
Sequence:
MSTATTVAPAGIPATPGPVNPPPPEVSNPSKPGRKTNQLQYMQNVVVKTLWKHQFAWPFYQPVDAIKLNLPDYHKIIKNPMDMGTIKKRLENNYYWSASECMQDFNTMFTNCYIYNKPTDDIVLMAQALEKIFLQKVAQMPQEEVELLPPAPKGKGRKPAAGAQSAGTQQVAAVSSVSPATPFQSVPPTVSQTPVIAATPVPTITANVTSVPVPPAAAPPPPATPIVPVVPPTPPVVKKKGVKRKADTTTPTTSAITASRSESPPPLSDPKQAKVVARRESGGRPIKPPKKDLEDGEVPQHAGKKGKLSEHLRYCDSILREMLSKKHAAYAWPFYKPVDAEALELHDYHDIIKHPMDLSTVKRKMDGREYPDAQGFAADVRLMFSNCYKYNPPDHEVVAMARKLQDVFEMRFAKMPDEPVEAPALPAPAAPMVSKGAESSRSSEESSSDSGSSDSEEERATRLAELQEQLKAVHEQLAALSQAPVNKPKKKKEKKEKEKKKKDKEKEKEKHKVKAEEEKKAKVAPPAKQAQQKKAPAKKANSTTTAGRQLKKGGKQASASYDSEEEEEGLPMSYDEKRQLSLDINRLPGEKLGRVVHIIQSREPSLRDSNPDEIEIDFETLKPTTLRELERYVKSCLQKKQRKPFSASGKKQAAKSKEELAQEKKKELEKRLQDVSGQLSSSKKPARKEKPGSAPSGGPSRLSSSSSSESGSSSSSGSSSDSSDSE
  
Inhibitor
Name:
BDBM50441168
Synonyms:
CHEMBL2430873
Type:
Small organic molecule
Emp. Form.:
C20H19N5O2
Mol. Mass.:
361.3972
SMILES:
CCOC(=O)N[C@@H]1N=C(c2ccccc2)c2ccccc2-n2c(C)nnc12 |r,t:7|
Structure:
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