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Target
Bromodomain-containing protein 4 [1-477]
Ligand
BDBM445535
Substrate
n/a
Meas. Tech.
Time Resolved Fluorescence Resonance Energy Transfer (TR-FRET) Assay
IC50
<5±n/a nM
Citation
 Quesnelle, CA; Harikrishnan, LS; Hill, MD Tricyclic compounds as anticancer agents US Patent  US10683290 Publication Date 6/16/2020 
Target
Name:
Bromodomain-containing protein 4 [1-477]
Synonyms:
BRD4 | BRD4_HUMAN | Bromodomain-containing protein 4 (BRD4)(1-477) | HUNK1
Type:
Enzyme Catalytic Domain
Mol. Mass.:
52863.68
Organism:
Homo sapiens (Human)
Description:
O60885[1-477]
Residue:
475
Sequence:
MSAESGPGTRLRNLPVMGDGLETSQMSTTQAQAQPQPANAASTNPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTEETEIMIVQAKGRGRGRKETGTAKPGVSTVPNTTQASTPPQTQTPQPNPPPVQATPHPFPAVTPDLIVQTPVMTVVPPQPLQTPPPVPPQPQPPPAPAPQPVQSHPPIIAATPQPVKTKKGVKRKADTTTPTTIDPIHEPPSLPPEPKTTKLGQRRESSRPVKPPKKDVPDSQQHPAPEKSSKVSEQLKCCSGILKEMFAKKHAAYAWPFYKPVDVEALGLHDYCDIIKHPMDMSTIKSKLEAREYRDAQEFGADVRLMFSNCYKYNPPDHEVVAMARKLQDVFEMRFAKMPDEPEEPVVAVSSPAVPP
  
Inhibitor
Name:
BDBM445535
Synonyms:
5-{3-Methanesulfonyl-5-[(S)-oxan-4-yl(phenyl)methyl]-5H-pyrido[3,2-b]indol-7-yl}-4-(2H3)methyl-1-methyl-1H-1,2,3-triazole | US10683290, Example 27
Type:
Small organic molecule
Emp. Form.:
C28H29N5O3S
Mol. Mass.:
515.627
SMILES:
Cc1nnn(C)c1-c1ccc2c(c1)n([C@@H](C1CCOCC1)c1ccccc1)c1cc(cnc21)S(C)(=O)=O
Structure:
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