Target
Bromodomain-containing protein 4 [75-147]
Ligand
BDBM333420
Substrate
n/a
Meas. Tech.
BRD4 AlphaScreen Assay
IC50
<100±n/a nM
Citation
 Yue, EWCombs, APBuesking, AW Bicyclic heterocycles as bet protein inhibitors US Patent  US9737516 Publication Date 8/22/2017 
Target
Name:
Bromodomain-containing protein 4 [75-147]
Synonyms:
BRD4 | BRD4_HUMAN | Bromo domain 1 | Bromodomain-containing protein 4 (BD1) | Bromodomain-containing protein 4 (BRD4) Bromo 1 | Bromodomain-containing protein 4 (BRD4)(BD1) | Bromodomain-containing protein 4 (BRD4)(Bromo 1) | Bromodomain-containing protein 4 Bromo 1 domain(BRD4 BD1) | Bromodomain-containing protein 4 Bromodomain 1 (BRD4-1) | Bromodomain-containing protein 4 Domain 1 | HUNK1
Type:
n/a
Mol. Mass.:
8856.55
Organism:
Homo sapiens (Human)
Description:
BD1 (75-147 aa) of O60885
Residue:
73
Sequence:
WKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIV
  
Inhibitor
Name:
BDBM333420
Synonyms:
4-[5-(Cyclobutylmethoxy)-1-benzyl-1H-benzimidazol-6-yl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one and 4-[6-(Cyclobutylmethoxy)-1-benzyl-1H-benzimidazol-5-yl]-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one | US9737516, Example 16 | US9737516, Example 17
Type:
Small organic molecule
Emp. Form.:
C27H26N4O2
Mol. Mass.:
438.5209
SMILES:
Cn1cc(-c2cc3n(Cc4ccccc4)cnc3cc2OCC2CCC2)c2cc[nH]c2c1=O
Structure:
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