| Reaction Details |
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 | Report a problem with these data |
| Target | Transcription activator BRG1 |
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| Ligand | BDBM50591346 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_2200139 (CHEMBL5112655) |
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| Kd | 142000±n/a nM |
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| Citation |  Shishodia, S; Nuņez, R; Strohmier, BP; Bursch, KL; Goetz, CJ; Olp, MD; Jensen, DR; Fenske, TG; Ordonez-Rubiano, SC; Blau, ME; Roach, MK; Peterson, FC; Volkman, BF; Dykhuizen, EC; Smith, BC Selective and Cell-Active PBRM1 Bromodomain Inhibitors Discovered through NMR Fragment Screening. J Med Chem65:13714-13735 (2022) [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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| BDBM50591346 |
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| n/a |
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| Name | BDBM50591346 |
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| Synonyms: | CHEMBL5188924 |
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| Type | Small organic molecule |
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| Emp. Form. | C14H10ClFN2O |
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| Mol. Mass. | 276.693 |
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| SMILES | Fc1cccc(Cl)c1C1NC(=O)c2ccccc2N1 |
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| Structure | 
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