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Target
Probable global transcription activator SNF2L2
Ligand
BDBM50469333
Substrate
n/a
Meas. Tech.
ChEMBL_1803941 (CHEMBL4276233)
IC50
60±n/a nM
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 Chem 61:10155-10172 (2018) [PubMed]  Article 
Target
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:
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQLQQKQSRISPIQKPQGLDPVEILQEREYRLQARIAHRIQELENLPGSLPPDLRTKATVELKALRLLNFQRQLRQEVVACMRRDTTLETALNSKAYKRSKRQTLREARMTEKLEKQQKIEQERKRRQKHQEYLNSILQHAKDFKEYHRSVAGKIQKLSKAVATWHANTEREQKKETERIEKERMRRLMAEDEEGYRKLIDQKKDRRLAYLLQQTDEYVANLTNLVWEHKQAQAAKEKKKRRRRKKKAEENAEGGESALGPDGEPIDESSQMSDLPVKVTHTETGKVLFGPEAPKASQLDAWLEMNPGYEVAPRSDSEESDSDYEEEDEEEESSRQETEEKILLDPNSEEVSEKDAKQIIETAKQDVDDEYSMQYSARGSQSYYTVAHAISERVEKQSALLINGTLKHYQLQGLEWMVSLYNNNLNGILADEMGLGKTIQTIALITYLMEHKRLNGPYLIIVPLSTLSNWTYEFDKWAPSVVKISYKGTPAMRRSLVPQLRSGKFNVLLTTYEYIIKDKHILAKIRWKYMIVDEGHRMKNHHCKLTQVLNTHYVAPRRILLTGTPLQNKLPELWALLNFLLPTIFKSCSTFEQWFNAPFAMTGERVDLNEEETILIIRRLHKVLRPFLLRRLKKEVESQLPEKVEYVIKCDMSALQKILYRHMQAKGILLTDGSEKDKKGKGGAKTLMNTIMQLRKICNHPYMFQHIEESFAEHLGYSNGVINGAELYRASGKFELLDRILPKLRATNHRVLLFCQMTSLMTIMEDYFAFRNFLYLRLDGTTKSEDRAALLKKFNEPGSQYFIFLLSTRAGGLGLNLQAADTVVIFDSDWNPHQDLQAQDRAHRIGQQNEVRVLRLCTVNSVEEKILAAAKYKLNVDQKVIQAGMFDQKSSSHERRAFLQAILEHEEENEEEDEVPDDETLNQMIARREEEFDLFMRMDMDRRREDARNPKRKPRLMEEDELPSWIIKDDAEVERLTCEEEEEKIFGRGSRQRRDVDYSDALTEKQWLRAIEDGNLEEMEEEVRLKKRKRRRNVDKDPAKEDVEKAKKRRGRPPAEKLSPNPPKLTKQMNAIIDTVINYKDRCNVEKVPSNSQLEIEGNSSGRQLSEVFIQLPSRKELPEYYELIRKPVDFKKIKERIRNHKYRSLGDLEKDVMLLCHNAQTFNLEGSQIYEDSIVLQSVFKSARQKIAKEEESEDESNEEEEEEDEEESESEAKSVKVKIKLNKKDDKGRDKGKGKKRPNRGKAKPVVSDFDSDEEQDEREQSEGSGTDDE
  
Inhibitor
Name:
BDBM50469333
Synonyms:
CHEMBL4290175
Type:
Small organic molecule
Emp. Form.:
C12H8ClF3N4O
Mol. Mass.:
316.666
SMILES:
FC(F)(F)c1cc(NC(=O)Nc2ccnc(Cl)c2)ccn1
Structure:
Search PDB for entries with ligand similarity: