| Reaction Details |
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 | Report a problem with these data |
| Target | Transcription activator BRG1 |
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| Ligand | BDBM50558065 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_2061751 (CHEMBL4717004) |
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| IC50 | >15000±n/a nM |
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| Citation |  Taylor, AM; Vaswani, RG; Gehling, VS; Hewitt, MC; Leblanc, Y; Audia, JE; Bellon, S; Cummings, RT; Côté, A; Harmange, JC; Jayaram, H; Joshi, S; Lora, JM; Mertz, JA; Neiss, A; Pardo, E; Nasveschuk, CG; Poy, F; Sandy, P; Setser, JW; Sims, RJ; Tang, Y; Albrecht, BK Discovery of Benzotriazolo[4,3-d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains. ACS Med Chem Lett7:145-50 (2016) [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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| BDBM50558065 |
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| n/a |
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| Name | BDBM50558065 |
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| Synonyms: | CHEMBL4780530 |
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| Type | Small organic molecule |
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| Emp. Form. | C23H21ClN6 |
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| Mol. Mass. | 416.906 |
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| SMILES | C[C@@H]1CN(c2ccc(Cl)cc2)c2cc(ccc2-n2c(C)nnc12)-c1ccc(N)nc1 |r| |
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| Structure | 
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