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Target
Bromodomain-containing protein 4 [49-170]
Ligand
BDBM480605
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:
BDBM480605
Synonyms:
1-(3-(1,3-dimethyl-1H- pyrazol-4-yl)isoquinolin-8- yl)-5,7-dimethyl-3- (tetrahydro-2H-pyran-4-yl)- 7,8-dihydroimidazo[1,5-a] pyrazin-6(5H)-one | US10899769, Example 87 | US10899769, Example 88
Type:
Small organic molecule
Emp. Form.:
C27H30N6O2
Mol. Mass.:
470.5661
SMILES:
CC1C(=O)N(C)Cc2c(nc(C3CCOCC3)n12)-c1cccc2cc(ncc12)-c1cn(C)nc1C
Structure:
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