Ki Summary

Reaction Details

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Target

Bromodomain-containing protein 4

Ligand

BDBM390847

Substrate/Competitor

n/a

Meas. Tech.

TR-FRET Assay (BD1: amino acids K57-E168)

4.60±n/a nM

Citation

Dai, Y; Fidanze, SD; Hasvold, L; Holms, J; Liu, D; McClellan, W; McDaniel, K; Marjanovic, J; Sheppard, G; Wang, L Bromodomain inhibitors US Patent US9957263 Publication Date 5/1/2018

More Info.:

Get all data from this article, Assay Method

Bromodomain-containing protein 4

Name:

Bromodomain-containing protein 4

Synonyms:

BRD4 | BRD4_HUMAN | Bromodomain-containing protein 4 (BRD4) | HUNK1 | Protein HUNK1

Type:

Protein

Mol. Mass.:

152264.84

Organism:

Homo sapiens (Human)

Description:

O60885

Residue:

1362

Sequence:

MSAESGPGTRLRNLPVMGDGLETSQMSTTQAQAQPQPANAASTNPPPPETSNPNKPKRQT
NQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYW
NAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTEETEIMIVQAKGRG
RGRKETGTAKPGVSTVPNTTQASTPPQTQTPQPNPPPVQATPHPFPAVTPDLIVQTPVMT
VVPPQPLQTPPPVPPQPQPPPAPAPQPVQSHPPIIAATPQPVKTKKGVKRKADTTTPTTI
DPIHEPPSLPPEPKTTKLGQRRESSRPVKPPKKDVPDSQQHPAPEKSSKVSEQLKCCSGI
LKEMFAKKHAAYAWPFYKPVDVEALGLHDYCDIIKHPMDMSTIKSKLEAREYRDAQEFGA
DVRLMFSNCYKYNPPDHEVVAMARKLQDVFEMRFAKMPDEPEEPVVAVSSPAVPPPTKVV
APPSSSDSSSDSSSDSDSSTDDSEEERAQRLAELQEQLKAVHEQLAALSQPQQNKPKKKE
KDKKEKKKEKHKRKEEVEENKKSKAKEPPPKKTKKNNSSNSNVSKKEPAPMKSKPPPTYE
SEEEDKCKPMSYEEKRQLSLDINKLPGEKLGRVVHIIQSREPSLKNSNPDEIEIDFETLK
PSTLRELERYVTSCLRKKRKPQAEKVDVIAGSSKMKGFSSSESESSSESSSSDSEDSETE
MAPKSKKKGHPGREQKKHHHHHHQQMQQAPAPVPQQPPPPPQQPPPPPPPQQQQQPPPPP
PPPSMPQQAAPAMKSSPPPFIATQVPVLEPQLPGSVFDPIGHFTQPILHLPQPELPPHLP
QPPEHSTPPHLNQHAVVSPPALHNALPQQPSRPSNRAAALPPKPARPPAVSPALTQTPLL
PQPPMAQPPQVLLEDEEPPAPPLTSMQMQLYLQQLQKVQPPTPLLPSVKVQSQPPPPLPP
PPHPSVQQQLQQQPPPPPPPQPQPPPQQQHQPPPRPVHLQPMQFSTHIQQPPPPQGQQPP
HPPPGQQPPPPQPAKPQQVIQHHHSPRHHKSDPYSTGHLREAPSPLMIHSPQMSQFQSLT
HQSPPQQNVQPKKQELRAASVVQPQPLVVVKEEKIHSPIIRSEPFSPSLRPEPPKHPESI
KAPVHLPQRPEMKPVDVGRPVIRPPEQNAPPPGAPDKDKQKQEPKTPVAPKKDLKIKNMG
SWASLVQKHPTTPSSTAKSSSDSFEQFRRAAREKEEREKALKAQAEHAEKEKERLRQERM
RSREDEDALEQARRAHEEARRRQEQQQQQRQEQQQQQQQQAAAVAAAATPQAQSSQPQSM
LDQQRELARKREQERRRREAMAATIDMNFQSDLLSIFEENLF

BDBM390847

n/a

Name

BDBM390847

Synonyms:

US9957263, Example 111

Type

Small organic molecule

Emp. Form.

C24H32N4O4S

Mol. Mass.

472.6

SMILES

COCCN[C@H]1CC[C@@H](CC1)Nc1ccc(cc1-c1cn(C)c(=O)c2[nH]ccc12)S(C)(=O)=O |r,wU:8.11,wD:5.4,(-9.34,-10.01,;-8,-9.24,;-8,-7.7,;-6.67,-6.93,;-6.67,-5.39,;-5.33,-4.62,;-4,-5.39,;-2.67,-4.62,;-2.67,-3.08,;-4,-2.31,;-5.33,-3.08,;-1.33,-2.31,;,-3.08,;,-4.62,;1.33,-5.39,;2.67,-4.62,;2.67,-3.08,;1.33,-2.31,;1.33,-.77,;2.67,,;2.67,1.54,;4,2.31,;1.33,2.31,;1.33,3.85,;,1.54,;-1.46,2.02,;-2.37,.77,;-1.46,-.48,;;4,-5.39,;4.77,-4.06,;5.33,-6.16,;3.23,-6.72,)|

Structure