Reaction Details |
| Report a problem with these data |
Target | Eukaryotic translation initiation factor 2-alpha kinase 3 |
---|
Ligand | BDBM50396549 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_862854 (CHEMBL2172956) |
---|
IC50 | 2.5±n/a nM |
---|
Citation | Axten, JM; Medina, JR; Feng, Y; Shu, A; Romeril, SP; Grant, SW; Li, WH; Heerding, DA; Minthorn, E; Mencken, T; Atkins, C; Liu, Q; Rabindran, S; Kumar, R; Hong, X; Goetz, A; Stanley, T; Taylor, JD; Sigethy, SD; Tomberlin, GH; Hassell, AM; Kahler, KM; Shewchuk, LM; Gampe, RT Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). J Med Chem55:7193-207 (2012) [PubMed] Article |
---|
More Info.: | Get all data from this article, Assay Method |
---|
|
Eukaryotic translation initiation factor 2-alpha kinase 3 |
---|
Name: | Eukaryotic translation initiation factor 2-alpha kinase 3 |
Synonyms: | E2AK3_HUMAN | EIF2AK3 | HsPEK | PEK | PERK | Pancreatic eIF2-alpha kinase | Pancreatic endoplasmic reticulum kinase (PERK) |
Type: | Enzyme |
Mol. Mass.: | 125190.66 |
Organism: | Homo sapiens (Human) |
Description: | Q9NZJ5 |
Residue: | 1116 |
Sequence: | MERAISPGLLVRALLLLLLLLGLAARTVAAGRARGLPAPTAEAAFGLGAAAAPTSATRVP
AAGAVAAAEVTVEDAEALPAAAGEQEPRGPEPDDETELRPRGRSLVIISTLDGRIAALDP
ENHGKKQWDLDVGSGSLVSSSLSKPEVFGNKMIIPSLDGALFQWDQDRESMETVPFTVES
LLESSYKFGDDVVLVGGKSLTTYGLSAYSGKVRYICSALGCRQWDSDEMEQEEDILLLQR
TQKTVRAVGPRSGNEKWNFSVGHFELRYIPDMETRAGFIESTFKPNENTEESKIISDVEE
QEAAIMDIVIKVSVADWKVMAFSKKGGHLEWEYQFCTPIASAWLLKDGKVIPISLFDDTS
YTSNDDVLEDEEDIVEAARGATENSVYLGMYRGQLYLQSSVRISEKFPSSPKALESVTNE
NAIIPLPTIKWKPLIHSPSRTPVLVGSDEFDKCLSNDKFSHEEYSNGALSILQYPYDNGY
YLPYYKRERNKRSTQITVRFLDNPHYNKNIRKKDPVLLLHWWKEIVATILFCIIATTFIV
RRLFHPHPHRQRKESETQCQTENKYDSVSGEANDSSWNDIKNSGYISRYLTDFEPIQCLG
RGGFGVVFEAKNKVDDCNYAIKRIRLPNRELAREKVMREVKALAKLEHPGIVRYFNAWLE
APPEKWQEKMDEIWLKDESTDWPLSSPSPMDAPSVKIRRMDPFATKEHIEIIAPSPQRSR
SFSVGISCDQTSSSESQFSPLEFSGMDHEDISESVDAAYNLQDSCLTDCDVEDGTMDGND
EGHSFELCPSEASPYVRSRERTSSSIVFEDSGCDNASSKEEPKTNRLHIGNHCANKLTAF
KPTSSKSSSEATLSISPPRPTTLSLDLTKNTTEKLQPSSPKVYLYIQMQLCRKENLKDWM
NGRCTIEERERSVCLHIFLQIAEAVEFLHSKGLMHRDLKPSNIFFTMDDVVKVGDFGLVT
AMDQDEEEQTVLTPMPAYARHTGQVGTKLYMSPEQIHGNSYSHKVDIFSLGLILFELLYP
FSTQMERVRTLTDVRNLKFPPLFTQKYPCEYVMVQDMLSPSPMERPEAINIIENAVFEDL
DFPGKTVLRQRSRSLSSSGTKHSRQSNNSHSPLPSN
|
|
|
BDBM50396549 |
---|
n/a |
---|
Name | BDBM50396549 |
Synonyms: | CHEMBL2171134 |
Type | Small organic molecule |
Emp. Form. | C23H17F2N3OS |
Mol. Mass. | 421.462 |
SMILES | Nc1nccc2scc(-c3ccc4N(CCc4c3)C(=O)Cc3cc(F)ccc3F)c12 |
Structure |
|