Target
Histone acetyltransferase KAT2A
Ligand
BDBM50506380
Substrate
n/a
Meas. Tech.
ChEMBL_1825679 (CHEMBL4325443)
IC50
>20000±n/a nM
Citation
 Yang, YZhang, RLi, ZMei, LWan, SDing, HChen, ZXing, JFeng, HHan, JJiang, HZheng, MLuo, CZhou, B Discovery of Highly Potent, Selective, and Orally Efficacious p300/CBP Histone Acetyltransferases Inhibitors. J Med Chem 63:1337-1360 (2020) [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:
BDBM50506380
Synonyms:
CHEMBL4587968
Type:
Small organic molecule
Emp. Form.:
C27H23F4N5O4
Mol. Mass.:
557.4962
SMILES:
Cn1cc(cn1)-c1ccc2c(CC[C@]22NC(=O)N(CC(=O)N3Cc4cc(F)ccc4OC[C@H]3C(F)(F)F)C2=O)c1 |r|
Structure:
Search PDB for entries with ligand similarity: