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Target
Bromodomain-containing protein 4 [42-168]
Ligand
BDBM318474
Substrate
n/a
Meas. Tech.
AlphaScreen Assay A1
IC50
<100±n/a nM
Citation
 Combs, AP; Sparks, RB; Maduskuie, Jr., TP; Rodgers, JD Tricyclic heterocycles as BET protein inhibitors US Patent  US10464947 Publication Date 11/5/2019 
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:
BDBM318474
Synonyms:
7-(3,5-Dimethylisoxazol-4-yl)-4-(1,3-thiazol-2-yl)-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2(1H)-one | US10464947, Example 21 | US11498926, Example 21 | US9624241, Example 21
Type:
Small organic molecule
Emp. Form.:
C17H14N4O3S
Mol. Mass.:
354.383
SMILES:
Cc1noc(C)c1-c1ccc2[nH]c(=O)n3C(COc1c23)c1nccs1 |(-.15,-5.8,;-1.48,-5.03,;-2.95,-5.51,;-3.85,-4.26,;-2.95,-3.02,;-3.72,-1.69,;-1.48,-3.49,;-.15,-2.72,;1.18,-3.49,;2.52,-2.72,;2.52,-1.18,;3.85,-.41,;2.72,1.13,;3.49,2.46,;1.18,1.13,;-.15,1.9,;-1.48,1.13,;-1.48,-.41,;-.15,-1.18,;1.18,-.41,;-.15,3.44,;1.1,4.34,;.62,5.8,;-.92,5.8,;-1.39,4.34,)|
Structure:
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