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Target
Histone acetyltransferase KAT2A
Ligand
BDBM50158627
Substrate
n/a
Meas. Tech.
ChEMBL_1771652 (CHEMBL4223764)
IC50
>80000±n/a nM
Citation
 Bennett, MJ; Wu, Y; Boloor, A; Matuszkiewicz, J; O'Connell, SM; Shi, L; Stansfield, RK; Del Rosario, JR; Veal, JM; Hosfield, DJ; Xu, J; Kaldor, SW; Stafford, JA; Betancort, JM Design, synthesis and biological evaluation of novel 4-phenylisoquinolinone BET bromodomain inhibitors. Bioorg Med Chem Lett 28:1811-1816 (2018) [PubMed]  Article 
Target
Name:
Histone acetyltransferase KAT2A
Synonyms:
GCN5 | GCN5 | GCN5L2 | General control of amino acid synthesis protein 5-like 2 | HGCN5 | Histone acetyltransferase GCN5 | Histone acetyltransferase KAT2A | Histone acetyltransferase KAT2A/KAT2B | HsGCN5 | KAT2A | KAT2A_HUMAN | Lysine acetyltransferase 2A | STAF97
Type:
PROTEIN
Mol. Mass.:
93956.22
Organism:
Homo sapiens (Human)
Description:
ChEMBL_100876
Residue:
837
Sequence:
MAEPSQAPTPAPAAQPRPLQSPAPAPTPTPAPSPASAPIPTPTPAPAPAPAAAPAGSTGTGGPGVGSGGAGSGGDPARPGLSQQQRASQRKAQVRGLPRAKKLEKLGVFSACKANETCKCNGWKNPKPPTAPRMDLQQPAANLSELCRSCEHPLADHVSHLENVSEDEINRLLGMVVDVENLFMSVHKEEDTDTKQVYFYLFKLLRKCILQMTRPVVEGSLGSPPFEKPNIEQGVLNFVQYKFSHLAPRERQTMFELSKMFLLCLNYWKLETPAQFRQRSQAEDVATYKVNYTRWLCYCHVPQSCDSLPRYETTHVFGRSLLRSIFTVTRRQLLEKFRVEKDKLVPEKRTLILTHFPKFLSMLEEEIYGANSPIWESGFTMPPSEGTQLVPRPASVSAAVVPSTPIFSPSMGGGSNSSLSLDSAGAEPMPGEKRTLPENLTLEDAKRLRVMGDIPMELVNEVMLTITDPAAMLGPETSLLSANAARDETARLEERRGIIEFHVIGNSLTPKANRRVLLWLVGLQNVFSHQLPRMPKEYIARLVFDPKHKTLALIKDGRVIGGICFRMFPTQGFTEIVFCAVTSNEQVKGYGTHLMNHLKEYHIKHNILYFLTYADEYAIGYFKKQGFSKDIKVPKSRYLGYIKDYEGATLMECELNPRIPYTELSHIIKKQKEIIKKLIERKQAQIRKVYPGLSCFKEGVRQIPVESVPGIRETGWKPLGKEKGKELKDPDQLYTTLKNLLAQIKSHPSAWPFMEPVKKSEAPDYYEVIRFPIDLKTMTERLRSRYYVTRKLFVADLQRVIANCREYNPPDSEYCRCASALEKFFYFKLKEGGLIDK
  
Inhibitor
Name:
BDBM50158627
Synonyms:
CHEMBL3787482 | US10023592, Example 81
Type:
Small organic molecule
Emp. Form.:
C24H25N3O4S
Mol. Mass.:
451.538
SMILES:
CCOc1ccc(cc1-c1cn(C)c(=O)c2ccc(cc12)-c1cnn(C)c1)S(=O)(=O)CC
Structure:
Search PDB for entries with ligand similarity: