Reaction Details
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Histone acetyltransferase KAT2A
Ligand
BDBM50579798
Substrate
n/a
Meas. Tech.
ChEMBL_2145448 (CHEMBL5029728)
IC50
>50000±n/a nM
Citation
Kanada, R; Suzuki, T; Murata, T; Miyazaki, M; Shimada, T; Kuroha, M; Minami, M; Higuchi, S; Tominaga, Y; Naito, H 4-Pyridone-3-carboxylic acid as a benzoic acid bioisostere: Design, synthesis, and evaluation of EP300/CBP histone acetyltransferase inhibitors. Bioorg Med Chem Lett 51:0 (2021) [PubMed] Article More Info.:
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:
BDBM50579798
Synonyms:
CHEMBL5080324
Type:
Small organic molecule
Emp. Form.:
C27H22N2O5S
Mol. Mass.:
486.539
SMILES:
COC1=C(Cc2ccc(s2)-c2cn(C)cc(C(O)=O)c2=O)C(=O)N(C1)c1ccc2ccccc2c1 |c:2|
Structure:
