Target
Probable global transcription activator SNF2L2
Ligand
BDBM646014
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:
BDBM646014
Synonyms:
(2S,4R)-4-hydroxy-1-((2S)-2-(2-(4-((2-(2- hydroxyphenyl)-5,6,6a,7,9,10-hexahydro-8H- pyrazino[1',2':4,5]pyrazino[2,3-c]pyridazin-8- yl)methyl)piperidin-1-yl)acetamido)-3,3- dimethylbutanoyl)-N-((S)-1-(4-(4- methylthiazol-5-yl)phenyl)ethyl)pyrrolidine- 2-carboxamide (Mixture of Diastereomers at *) | US20240018158, Example 3
Type:
Small organic molecule
Emp. Form.:
C46H60N10O5S
Mol. Mass.:
865.098
SMILES:
C[C@H](NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](NC(=O)CN1CCC(CN2CCN3C(CNc4nnc(cc34)-c3ccccc3O)C2)CC1)C(C)(C)C)c1ccc(cc1)-c1scnc1C |r|
Structure:
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