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TargetHistone acetyltransferase KAT2A
LigandBDBM50346552
Substrate/Competitorn/a
Meas. Tech.ChEMBL_2233609 (CHEMBL5147381)
IC50 47400±n/a nM
Citation Kanada, RKagoshima, YAsano, MSuzuki, TMurata, THaruta, MTakahashi, MUbukata, OHashimoto, KObata, KKihara, KKuroha, MBanjo, TTogashi, NSato, KYamamoto, YSuzuki, KIsoyama, TTominaga, YHiguchi, SNaito, H Discovery of EP300/CBP histone acetyltransferase inhibitors through scaffold hopping of 1,4-oxazepane ring. Bioorg Med Chem Lett66:0 (2022) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Histone acetyltransferase KAT2A
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:
MAEPSQAPTPAPAAQPRPLQSPAPAPTPTPAPSPASAPIPTPTPAPAPAPAAAPAGSTGT
GGPGVGSGGAGSGGDPARPGLSQQQRASQRKAQVRGLPRAKKLEKLGVFSACKANETCKC
NGWKNPKPPTAPRMDLQQPAANLSELCRSCEHPLADHVSHLENVSEDEINRLLGMVVDVE
NLFMSVHKEEDTDTKQVYFYLFKLLRKCILQMTRPVVEGSLGSPPFEKPNIEQGVLNFVQ
YKFSHLAPRERQTMFELSKMFLLCLNYWKLETPAQFRQRSQAEDVATYKVNYTRWLCYCH
VPQSCDSLPRYETTHVFGRSLLRSIFTVTRRQLLEKFRVEKDKLVPEKRTLILTHFPKFL
SMLEEEIYGANSPIWESGFTMPPSEGTQLVPRPASVSAAVVPSTPIFSPSMGGGSNSSLS
LDSAGAEPMPGEKRTLPENLTLEDAKRLRVMGDIPMELVNEVMLTITDPAAMLGPETSLL
SANAARDETARLEERRGIIEFHVIGNSLTPKANRRVLLWLVGLQNVFSHQLPRMPKEYIA
RLVFDPKHKTLALIKDGRVIGGICFRMFPTQGFTEIVFCAVTSNEQVKGYGTHLMNHLKE
YHIKHNILYFLTYADEYAIGYFKKQGFSKDIKVPKSRYLGYIKDYEGATLMECELNPRIP
YTELSHIIKKQKEIIKKLIERKQAQIRKVYPGLSCFKEGVRQIPVESVPGIRETGWKPLG
KEKGKELKDPDQLYTTLKNLLAQIKSHPSAWPFMEPVKKSEAPDYYEVIRFPIDLKTMTE
RLRSRYYVTRKLFVADLQRVIANCREYNPPDSEYCRCASALEKFFYFKLKEGGLIDK
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50346552
n/a
NameBDBM50346552
Synonyms:CHEMBL1797936
TypeSmall organic molecule
Emp. Form.C24H19N3O6
Mol. Mass.445.4242
SMILESCc1cc(-c2ccc(C=c3c(=C)[nH]n(-c4ccc(cc4)C(O)=O)c3=O)o2)c(cc1C)[N+]([O-])=O |w:8.7|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: