Reaction Details |
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Target | Histone acetyltransferase KAT2A |
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Ligand | BDBM220447 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1670375 (CHEMBL4020263) |
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Kd | >1000±n/a nM |
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Citation | McDaniel, KF; Wang, L; Soltwedel, T; Fidanze, SD; Hasvold, LA; Liu, D; Mantei, RA; Pratt, JK; Sheppard, GS; Bui, MH; Faivre, EJ; Huang, X; Li, L; Lin, X; Wang, R; Warder, SE; Wilcox, D; Albert, DH; Magoc, TJ; Rajaraman, G; Park, CH; Hutchins, CW; Shen, JJ; Edalji, RP; Sun, CC; Martin, R; Gao, W; Wong, S; Fang, G; Elmore, SW; Shen, Y; Kati, WM Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor. J Med Chem60:8369-8384 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Histone acetyltransferase KAT2A |
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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
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BDBM220447 |
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n/a |
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Name | BDBM220447 |
Synonyms: | US10633379, Compound X | US9296741, 36 |
Type | Small organic molecule |
Emp. Form. | C22H19F2N3O4S |
Mol. Mass. | 459.466 |
SMILES | CCS(=O)(=O)Nc1ccc(Oc2ccc(F)cc2F)c(c1)-c1cn(C)c(=O)c2[nH]ccc12 |
Structure |
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