Reaction Details |
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Target | Probable global transcription activator SNF2L2 |
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Ligand | BDBM50469323 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1803941 (CHEMBL4276233) |
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IC50 | 1100±n/a nM |
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Citation | Papillon, JPN; Nakajima, K; Adair, CD; Hempel, J; Jouk, AO; Karki, RG; Mathieu, S; Möbitz, H; Ntaganda, R; Smith, T; Visser, M; Hill, SE; Hurtado, FK; Chenail, G; Bhang, HC; Bric, A; Xiang, K; Bushold, G; Gilbert, T; Vattay, A; Dooley, J; Costa, EA; Park, I; Li, A; Farley, D; Lounkine, E; Yue, QK; Xie, X; Zhu, X; Kulathila, R; King, D; Hu, T; Vulic, K; Cantwell, J; Luu, C; Jagani, Z Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers. J Med Chem61:10155-10172 (2018) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Probable global transcription activator SNF2L2 |
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Name: | Probable global transcription activator SNF2L2 |
Synonyms: | ATP-dependent helicase SMARCA2 | BAF190B | BRG1-associated factor 190B | BRM | Protein brahma homolog | SMARCA2 | SMCA2_HUMAN | SNF2-alpha | SNF2A | SNF2L2 | SWI/SNF-related matrix-associated actin-dependent regulator of chromatin subfamily A member 2 | hBRM |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 181290.91 |
Organism: | Homo sapiens (Human) |
Description: | P51531 |
Residue: | 1590 |
Sequence: | MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTM
GSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGY
MSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLH
QLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQ
QQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAA
AVPGPSVPQPAPGQPSPVLQLQQKQSRISPIQKPQGLDPVEILQEREYRLQARIAHRIQE
LENLPGSLPPDLRTKATVELKALRLLNFQRQLRQEVVACMRRDTTLETALNSKAYKRSKR
QTLREARMTEKLEKQQKIEQERKRRQKHQEYLNSILQHAKDFKEYHRSVAGKIQKLSKAV
ATWHANTEREQKKETERIEKERMRRLMAEDEEGYRKLIDQKKDRRLAYLLQQTDEYVANL
TNLVWEHKQAQAAKEKKKRRRRKKKAEENAEGGESALGPDGEPIDESSQMSDLPVKVTHT
ETGKVLFGPEAPKASQLDAWLEMNPGYEVAPRSDSEESDSDYEEEDEEEESSRQETEEKI
LLDPNSEEVSEKDAKQIIETAKQDVDDEYSMQYSARGSQSYYTVAHAISERVEKQSALLI
NGTLKHYQLQGLEWMVSLYNNNLNGILADEMGLGKTIQTIALITYLMEHKRLNGPYLIIV
PLSTLSNWTYEFDKWAPSVVKISYKGTPAMRRSLVPQLRSGKFNVLLTTYEYIIKDKHIL
AKIRWKYMIVDEGHRMKNHHCKLTQVLNTHYVAPRRILLTGTPLQNKLPELWALLNFLLP
TIFKSCSTFEQWFNAPFAMTGERVDLNEEETILIIRRLHKVLRPFLLRRLKKEVESQLPE
KVEYVIKCDMSALQKILYRHMQAKGILLTDGSEKDKKGKGGAKTLMNTIMQLRKICNHPY
MFQHIEESFAEHLGYSNGVINGAELYRASGKFELLDRILPKLRATNHRVLLFCQMTSLMT
IMEDYFAFRNFLYLRLDGTTKSEDRAALLKKFNEPGSQYFIFLLSTRAGGLGLNLQAADT
VVIFDSDWNPHQDLQAQDRAHRIGQQNEVRVLRLCTVNSVEEKILAAAKYKLNVDQKVIQ
AGMFDQKSSSHERRAFLQAILEHEEENEEEDEVPDDETLNQMIARREEEFDLFMRMDMDR
RREDARNPKRKPRLMEEDELPSWIIKDDAEVERLTCEEEEEKIFGRGSRQRRDVDYSDAL
TEKQWLRAIEDGNLEEMEEEVRLKKRKRRRNVDKDPAKEDVEKAKKRRGRPPAEKLSPNP
PKLTKQMNAIIDTVINYKDRCNVEKVPSNSQLEIEGNSSGRQLSEVFIQLPSRKELPEYY
ELIRKPVDFKKIKERIRNHKYRSLGDLEKDVMLLCHNAQTFNLEGSQIYEDSIVLQSVFK
SARQKIAKEEESEDESNEEEEEEDEEESESEAKSVKVKIKLNKKDDKGRDKGKGKKRPNR
GKAKPVVSDFDSDEEQDEREQSEGSGTDDE
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BDBM50469323 |
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n/a |
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Name | BDBM50469323 |
Synonyms: | CHEMBL4290675 |
Type | Small organic molecule |
Emp. Form. | C11H9ClN4O |
Mol. Mass. | 248.668 |
SMILES | Clc1cc(NC(=O)Nc2ccncc2)ccn1 |
Structure |
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