Reaction Details Report a problem with these data
Target
Probable global transcription activator SNF2L2
Ligand
BDBM646012
Substrate
n/a
Meas. Tech.
SMARCA2 Bromodomain Binary and Ternary Binding Assay
IC50
550±n/a nM
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 
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:
BDBM646012
Synonyms:
(2S,4R)-4-hydroxy-N-[[4-(5-methyl-1,3- thiazol-4-yl)phenyl]methyl]-1-[(2S)-2-[[2-[4- (2-hydroxyphenyl)-1,5,6,8,12- pentazatricyclo[8.4.0.02,7]tetradeca-2,4,6- trien-12-yl]acetyl]amino]-3,3- dimethylbutanoyl]pyrrolidine-2-carboxamide (Diastereomer 1 - *) | US20240018158, Example 2a | US20240018158, Example 2b
Type:
Small organic molecule
Emp. Form.:
C39H47N9O5S
Mol. Mass.:
753.913
SMILES:
Cc1scnc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CN2CCN3C(CNc4nnc(cc34)-c3ccccc3O)C2)C(C)(C)C)cc1 |r|
Structure:
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