Target
Probable global transcription activator SNF2L2
Ligand
BDBM646015
Substrate
n/a
Meas. Tech.
SMARCA2 Bromodomain Binary and Ternary Binding Assay
IC50
<100±n/a nM
Citation
 Lin, HPitis, PLu, LCombs, 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:
BDBM646015
Synonyms:
(2S,4R)-4-hydroxy-1-((2R)-2-(3-(2-(2-(2- hydroxyphenyl)-5,6,6a,7,9,10-hexahydro-8H- pyrazino[1',2':4,5]pyrazino[2,3-c]pyridazin-8- yl)ethoxy)isoxazol-5-yl)-3-methylbutanoyl)- N-((S)-1-(4-(4-methyl-1lambda3,3lambda2-thiazol-5- yl)phenyl)ethyl)pyrrolidine-2-carboxamide (Mixture of Diastereomers at *) | US20240018158, Example 4
Type:
Small organic molecule
Emp. Form.:
C42H49N9O6S
Mol. Mass.:
807.96
SMILES:
CC(C)[C@@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(cc1)-c1scnc1C)c1cc(OCCN2CCN3C(CNc4nnc(cc34)-c3ccccc3O)C2)no1 |r,w:39.42|
Structure:
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