Reaction Details |
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Target | Bromodomain-containing protein 4 [75-147] |
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Ligand | BDBM391537 |
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Substrate/Competitor | n/a |
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Meas. Tech. | AlphaScreen Assay |
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IC50 | <100±n/a nM |
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Citation | Combs, AP; Maduskuie, Jr., TP; Falahatpisheh, N 1H-pyrrolo[2,3-c]pyridin-7(6H)-ones and pyrazolo[3,4-c]pyridin-7(6H)-ones as inhibitors of BET proteins US Patent US10472358 Publication Date 11/12/2019 |
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More Info.: | Get all data from this article, Assay Method |
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Bromodomain-containing protein 4 [75-147] |
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Name: | Bromodomain-containing protein 4 [75-147] |
Synonyms: | BRD4-BD1 |
Type: | Protein |
Mol. Mass.: | n/a |
Description: | n/a |
Components: | This complex has 2 components. |
Component 1 |
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
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Component 2 |
Name: | Bromodomain-containing protein 4 [75-147] |
Synonyms: | BRD4 | BRD4_HUMAN | Bromo domain 1 | Bromodomain-containing protein 4 (BD1) | Bromodomain-containing protein 4 (BRD4) Bromo 1 | Bromodomain-containing protein 4 (BRD4)(BD1) | Bromodomain-containing protein 4 (BRD4)(Bromo 1) | Bromodomain-containing protein 4 Bromo 1 domain(BRD4 BD1) | Bromodomain-containing protein 4 Bromodomain 1 (BRD4-1) | Bromodomain-containing protein 4 Domain 1 | HUNK1 |
Type: | n/a |
Mol. Mass.: | 8856.55 |
Organism: | Homo sapiens (Human) |
Description: | BD1 (75-147 aa) of O60885 |
Residue: | 73 |
Sequence: | WKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQECIQDFNTMFT
NCYIYNKPGDDIV
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BDBM391537 |
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n/a |
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Name | BDBM391537 |
Synonyms: | 2-isopropyl-8-(6-methyl-7- oxo-6,7-dihydro-1H- pyrrolo[2,3-c]pyridin-4-yl)-6- (morpholin-4-ylcarbonyl)-2H- 1,4-benzoxazin-3(4H)-one | US10472358, Example 33 | US10781209, Example 33 | US11702416, Example 33 | US9957268, Example 33 |
Type | Small organic molecule |
Emp. Form. | C24H26N4O5 |
Mol. Mass. | 450.487 |
SMILES | CC(C)C1Oc2c(NC1=O)cc(cc2-c1cn(C)c(=O)c2[nH]ccc12)C(=O)N1CCOCC1 |
Structure |
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