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Target
MAP kinase-activated protein kinase 3
Ligand
BDBM50315888
Substrate
n/a
Meas. Tech.
ChEMBL_625037 (CHEMBL1109705)
IC50
>1000±n/a nM
Citation
Fidanze, SD; Erickson, SA; Wang, GT; Mantei, R; Clark, RF; Sorensen, BK; Bamaung, NY; Kovar, P; Johnson, EF; Swinger, KK; Stewart, KD; Zhang, Q; Tucker, LA; Pappano, WN; Wilsbacher, JL; Wang, J; Sheppard, GS; Bell, RL; Davidsen, SK; Hubbard, RD Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases. Bioorg Med Chem Lett 20:2452-5 (2010) [PubMed] Article
More Info.:
Target
Name:
MAP kinase-activated protein kinase 3
Synonyms:
3pK | Chromosome 3p kinase | MAP kinase-activated protein kinase 3 (MAPKAP-K3) | MAPK-Activated Protein Kinase 3 (MK3) | MAPK-activated protein kinase 3 | MAPK3_HUMAN | MAPKAP kinase 3 | MAPKAPK-3 | MAPKAPK3
Type:
Serine/threonine-protein kinase
Mol. Mass.:
42991.57
Organism:
Homo sapiens (Human)
Description:
Recombinant MAPKAPK3 was phosphorylated by incubation with active p38alpha before assays.
Residue:
382
Sequence:
MDGETAEEQGGPVPPPVAPGGPGLGGAPGGRREPKKYAVTDDYQLSKQVLGLGVNGKVLECFHRRTGQKCALKLLYDSPKARQEVDHHWQASGGPHIVCILDVYENMHHGKRCLLIIMECMEGGELFSRIQERGDQAFTEREAAEIMRDIGTAIQFLHSHNIAHRDVKPENLLYTSKEKDAVLKLTDFGFAKETTQNALQTPCYTPYYVAPEVLGPEKYDKSCDMWSLGVIMYILLCGFPPFYSNTGQAISPGMKRRIRLGQYGFPNPEWSEVSEDAKQLIRLLLKTDPTERLTITQFMNHPWINQSMVVPQTPLHTARVLQEDKDHWDEVKEEMTSALATMRVDYDQVKIKDLKTSNNRLLNKRRKKQAGSSSASQGCNNQ
Inhibitor
Name:
BDBM50315888
Synonyms:
CHEMBL1090360 | N-(3-(5-(2-(3-morpholinophenylamino)pyrimidin-4-yl)imidazo[2,1-b]thiazol-6-yl)phenyl)-2-phenylacetamide
Type:
Small organic molecule
Emp. Form.:
C33H29N7O2S
Mol. Mass.:
587.694
SMILES:
O=C(Cc1ccccc1)Nc1cccc(c1)-c1nc2sccn2c1-c1ccnc(Nc2cccc(c2)N2CCOCC2)n1