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Target
Histone acetyltransferase KAT2A
Ligand
BDBM50269847
Substrate
n/a
Meas. Tech.
ChEMBL_1707380 (CHEMBL4058613)
IC50
>20000±n/a nM
Citation
 Romero, FA; Murray, J; Lai, KW; Tsui, V; Albrecht, BK; An, L; Beresini, MH; de Leon Boenig, G; Bronner, SM; Chan, EW; Chen, KX; Chen, Z; Choo, EF; Clagg, K; Clark, K; Crawford, TD; Cyr, P; de Almeida Nagata, D; Gascoigne, KE; Grogan, JL; Hatzivassiliou, G; Huang, W; Hunsaker, TL; Kaufman, S; Koenig, SG; Li, R; Li, Y; Liang, X; Liao, J; Liu, W; Ly, J; Maher, J; Masui, C; Merchant, M; Ran, Y; Taylor, AM; Wai, J; Wang, F; Wei, X; Yu, D; Zhu, BY; Zhu, X; Magnuson, S GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP). J Med Chem 60:9162-9183 (2017) [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:
BDBM50269847
Synonyms:
CHEMBL4097025
Type:
Small organic molecule
Emp. Form.:
C27H33F2N7O2
Mol. Mass.:
525.5934
SMILES:
CNC(=O)N1CCc2c(C1)c(nn2C1CCOCC1)N1CCCc2cc(-c3cnn(C)c3)c(cc12)C(F)F
Structure:
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