Target
Histone acetyltransferase KAT2A
Ligand
BDBM342597
Substrate
n/a
Meas. Tech.
ChEBML_1687836
IC50
>1000±n/a nM
Citation
 Hasvold, LASheppard, GSWang, LFidanze, SDLiu, DPratt, JKMantei, RAWada, CKHubbard, RShen, YLin, XHuang, XWarder, SEWilcox, DLi, LBuchanan, FGSmithee, LAlbert, DHMagoc, TJPark, CHPetros, AMPanchal, SCSun, CKovar, PSoni, NBElmore, SWKati, WMMcDaniel, KF Methylpyrrole inhibitors of BET bromodomains. Bioorg Med Chem Lett 27:2225-2233 (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:
BDBM342597
Synonyms:
N-[3-(3-methyl-4-oxo-4,5,6,7-tetrahydro-2H-isoindol-1-yl)-4-phenoxyphenyl]methanesulfonamide | US9776990, Example 40
Type:
Small organic molecule
Emp. Form.:
C22H22N2O4S
Mol. Mass.:
410.486
SMILES:
Cc1[nH]c(c2CCCC(=O)c12)-c1cc(NS(C)(=O)=O)ccc1Oc1ccccc1
Structure:
Search PDB for entries with ligand similarity: