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Target
Bromodomain-containing protein 4 [42-168]
Ligand
BDBM391581
Substrate
n/a
Meas. Tech.
BRD4 AlphaScreen Assay
IC50
<100±n/a nM
Citation
 Combs, AP; Maduskuie, Jr., TP; Falahatpisheh, N 1H-pyrrolo[2,3,c]pyridin-7(6H)-ones and pyrazolo[3,4-c]pyridin-7(6H)-ones as inhibitors of BET proteins US Patent  US9957268 Publication Date 5/1/2018 
Target
Name:
Bromodomain-containing protein 4 [42-168]
Synonyms:
BRD4 | BRD4 BD1 (aa 42-168) | BRD4_HUMAN | Bromodomain-containing protein 4 Bromo Domain 1 | HUNK1
Type:
Enzyme Catalytic Domain
Mol. Mass.:
15054.68
Organism:
Homo sapiens (Human)
Description:
O60885[42-168]
Residue:
127
Sequence:
STNPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTEE
  
Inhibitor
Name:
BDBM391581
Synonyms:
N,N,2,2,4-pentamethyl-8-(6- methyl-7-oxo-6,7-dihydro- 1H-pyrrolo[2,3-c]pyridin-4- yl)-3-oxo-3,4-dihydro-2H-1,4- benzoxazine-6-sulfonamide | US10472358, Example 69 | US10781209, Example 70 | US11059821, Example 69 | US11702416, Example 69 | US9957268, Example 69
Type:
Small organic molecule
Emp. Form.:
C21H24N4O5S
Mol. Mass.:
444.504
SMILES:
CN(C)S(=O)(=O)c1cc2N(C)C(=O)C(C)(C)Oc2c(c1)-c1cn(C)c(=O)c2[nH]ccc12
Structure:
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