| Reaction Details |
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 | Report a problem with these data |
| Target | Transcription activator BRG1 |
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| Ligand | BDBM220447 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1670379 (CHEMBL4020267) |
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| Kd | >1000±n/a nM |
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| Citation |  McDaniel, KF; Wang, L; Soltwedel, T; Fidanze, SD; Hasvold, LA; Liu, D; Mantei, RA; Pratt, JK; Sheppard, GS; Bui, MH; Faivre, EJ; Huang, X; Li, L; Lin, X; Wang, R; Warder, SE; Wilcox, D; Albert, DH; Magoc, TJ; Rajaraman, G; Park, CH; Hutchins, CW; Shen, JJ; Edalji, RP; Sun, CC; Martin, R; Gao, W; Wong, S; Fang, G; Elmore, SW; Shen, Y; Kati, WM Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor. J Med Chem60:8369-8384 (2017) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Transcription activator BRG1 |
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| Name: | Transcription activator BRG1 |
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| Synonyms: | ATP-dependent helicase SMARCA4 | BAF190A | BRG1 | BRG1-associated factor 190A | Mitotic growth and transcription activator | Protein BRG-1 | Protein brahma homolog 1 | SMARCA4 | SMCA4_HUMAN | SNF2-beta | SNF2B | SNF2L4 | SWI/SNF-related matrix-associated actin-dependent regulator of chromatin subfamily A member 4 |
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| Type: | PROTEIN |
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| Mol. Mass.: | 184666.66 |
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| Organism: | Homo sapiens (Human) |
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| Description: | ChEMBL_107968 |
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| Residue: | 1647 |
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| Sequence: | MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQG
PGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGY
PSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQL
RAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGP
GPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQ
KLIPPQPTGRPSPAPPAVPPAASPVMPPQTQSPGQPAQPAPMVPLHQKQSRITPIQKPRG
LDPVEILQEREYRLQARIAHRIQELENLPGSLAGDLRTKATIELKALRLLNFQRQLRQEV
VVCMRRDTALETALNAKAYKRSKRQSLREARITEKLEKQQKIEQERKRRQKHQEYLNSIL
QHAKDFKEYHRSVTGKIQKLTKAVATYHANTEREQKKENERIEKERMRRLMAEDEEGYRK
LIDQKKDKRLAYLLQQTDEYVANLTELVRQHKAAQVAKEKKKKKKKKKAENAEGQTPAIG
PDGEPLDETSQMSDLPVKVIHVESGKILTGTDAPKAGQLEAWLEMNPGYEVAPRSDSEES
GSEEEEEEEEEEQPQAAQPPTLPVEEKKKIPDPDSDDVSEVDARHIIENAKQDVDDEYGV
SQALARGLQSYYAVAHAVTERVDKQSALMVNGVLKQYQIKGLEWLVSLYNNNLNGILADE
MGLGKTIQTIALITYLMEHKRINGPFLIIVPLSTLSNWAYEFDKWAPSVVKVSYKGSPAA
RRAFVPQLRSGKFNVLLTTYEYIIKDKHILAKIRWKYMIVDEGHRMKNHHCKLTQVLNTH
YVAPRRLLLTGTPLQNKLPELWALLNFLLPTIFKSCSTFEQWFNAPFAMTGEKVDLNEEE
TILIIRRLHKVLRPFLLRRLKKEVEAQLPEKVEYVIKCDMSALQRVLYRHMQAKGVLLTD
GSEKDKKGKGGTKTLMNTIMQLRKICNHPYMFQHIEESFSEHLGFTGGIVQGLDLYRASG
KFELLDRILPKLRATNHKVLLFCQMTSLMTIMEDYFAYRGFKYLRLDGTTKAEDRGMLLK
TFNEPGSEYFIFLLSTRAGGLGLNLQSADTVIIFDSDWNPHQDLQAQDRAHRIGQQNEVR
VLRLCTVNSVEEKILAAAKYKLNVDQKVIQAGMFDQKSSSHERRAFLQAILEHEEQDESR
HCSTGSGSASFAHTAPPPAGVNPDLEEPPLKEEDEVPDDETVNQMIARHEEEFDLFMRMD
LDRRREEARNPKRKPRLMEEDELPSWIIKDDAEVERLTCEEEEEKMFGRGSRHRKEVDYS
DSLTEKQWLKAIEEGTLEEIEEEVRQKKSSRKRKRDSDAGSSTPTTSTRSRDKDDESKKQ
KKRGRPPAEKLSPNPPNLTKKMKKIVDAVIKYKDSSSGRQLSEVFIQLPSRKELPEYYEL
IRKPVDFKKIKERIRNHKYRSLNDLEKDVMLLCQNAQTFNLEGSLIYEDSIVLQSVFTSV
RQKIEKEDDSEGEESEEEEEGEEEGSESESRSVKVKIKLGRKEKAQDRLKGGRRRPSRGS
RAKPVVSDDDSEEEQEEDRSGSGSEED
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| BDBM220447 |
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| n/a |
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| Name | BDBM220447 |
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| Synonyms: | US10633379, Compound X | US9296741, 36 |
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| Type | Small organic molecule |
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| Emp. Form. | C22H19F2N3O4S |
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| Mol. Mass. | 459.466 |
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| SMILES | CCS(=O)(=O)Nc1ccc(Oc2ccc(F)cc2F)c(c1)-c1cn(C)c(=O)c2[nH]ccc12 |
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| Structure | 
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