Reaction Details |
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Target | Transcription activator BRG1 |
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Ligand | BDBM646010 |
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Substrate/Competitor | n/a |
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Meas. Tech. | SMARCA4 Bromodomain Binary and Ternary Binding Assay |
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IC50 | <100±n/a nM |
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Citation | Lin, H; Pitis, P; Lu, L; Combs, AP BRM TARGETING COMPOUNDS AND ASSOCIATED METHODS OF USE US Patent US20240018158 Publication Date 1/18/2024 |
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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 |
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 |
Type: | PROTEIN |
Mol. Mass.: | 184666.66 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_107968 |
Residue: | 1647 |
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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BDBM646010 |
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n/a |
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Name | BDBM646010 |
Synonyms: | (2S,4R)-4-hydroxy-1-((2S)-2-(2-(2-(2- hydroxyphenyl)-5,6,6a,7,9,10-hexahydro-8H- pyrazino[1',2':4,5]pyrazino[2,3-c]pyridazin-8- yl)acetamido)-3,3-dimethylbutanoyl)-N-((S)- 1-(4-(4-methylthiazol-5- yl)phenyl)ethyl)pyrrolidine-2-carboxamide (Diastereomer 1 - *) | US20240018158, Example 1a | US20240018158, Example 1b |
Type | Small organic molecule |
Emp. Form. | C40H49N9O5S |
Mol. Mass. | 767.939 |
SMILES | C[C@H](NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](NC(=O)CN1CCN2C(CNc3nnc(cc23)-c2ccccc2O)C1)C(C)(C)C)c1ccc(cc1)-c1scnc1C |r| |
Structure |
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