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Target
Bromodomain-containing protein 4 [49-170]
Ligand
BDBM480562
Substrate
n/a
Meas. Tech.
AlphaScreen Assay
IC50
2.00±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
More Info.:
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:
BDBM480562
Synonyms:
3-(5-(3-Cyclopropyl-5,7-dimethyl-6-oxo-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazin-1-yl)-3-(difluoromethyl)quinolin-2-yl)-1,2,4-thiadiazol-5(4H)-one | US10899769, Example 46
Type:
Small organic molecule
Emp. Form.:
C23H20F2N6O2S
Mol. Mass.:
482.506
SMILES:
CC1C(=O)N(C)Cc2c(nc(C3CC3)n12)-c1cccc2nc(-c3nsc(=O)[nH]3)c(cc12)C(F)F