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Target
Bromodomain-containing protein 4 [49-170]
Ligand
BDBM480607
Substrate
n/a
Meas. Tech.
AlphaScreen Assay
IC50
1.000±n/a nM
Citation
 Le, K; Soth, MJ; Liu, G; Jones, P; Cross, JB; Mcafoos, TJ; Carroll, CL; Lewis, RT Imidazopiperazinone inhibitors of transcription activating proteins US Patent  US10899769 Publication Date 1/26/2021 
Target
Name:
Bromodomain-containing protein 4 [49-170]
Synonyms:
BRD4 | BRD4-BD1 | BRD4-BD1 (aa 49-170) | BRD4_HUMAN | Bromodomain containing 4 (aa 49-170) | Bromodomain-containing protein 4 (BRD4) | Bromodomain-containing protein 4 (BRD4)(49-170) | Bromodomain-containing protein 4 (BRD4)(BD1) | HUNK1
Type:
Enzyme Catalytic Domain
Mol. Mass.:
14593.14
Organism:
Homo sapiens (Human)
Description:
aa 49-170 (BRD4-BD1)
Residue:
122
Sequence:
ETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTEETE
  
Inhibitor
Name:
BDBM480607
Synonyms:
(R)-1-(3-(difluoromethyl)- 2-(1-methyl-1H-pyrazol-3- yl)quinolin-5-yl)-5,7- dimethyl-3-(tetrahydro-2H- pyran-4-yl)-7,8- dihydroimidazo[1,5-a] pyrazin-6(5H)-one | US10899769, Example 89a
Type:
Small organic molecule
Emp. Form.:
C27H28F2N6O2
Mol. Mass.:
506.547
SMILES:
C[C@@H]1C(=O)N(C)Cc2c(nc(C3CCOCC3)n12)-c1cccc2nc(-c3ccn(C)n3)c(cc12)C(F)F |r|
Structure:
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