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Target
MAP kinase-activated protein kinase 3
Ligand
BDBM50305006
Substrate
n/a
Meas. Tech.
ChEMBL_606944 (CHEMBL1072687)
IC50
3800±n/a nM
Citation
 Harris, CM; Ericsson, AM; Argiriadi, MA; Barberis, C; Borhani, DW; Burchat, A; Calderwood, DJ; Cunha, GA; Dixon, RW; Frank, KE; Johnson, EF; Kamens, J; Kwak, S; Li, B; Mullen, KD; Perron, DC; Wang, L; Wishart, N; Wu, X; Zhang, X; Zmetra, TR; Talanian, RV 2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization. Bioorg Med Chem Lett 20:334-7 (2010) [PubMed]  Article 
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:
BDBM50305006
Synonyms:
5-(2-aminoethyl)-7-(7-(benzo[b]thiophen-2-yl)-1H-indazol-5-yl)-5H-pyrrolo[3,2-d]pyrimidin-2-amine | CHEMBL590109
Type:
Small organic molecule
Emp. Form.:
C23H19N7S
Mol. Mass.:
425.509
SMILES:
NCCn1cc(-c2cc(-c3cc4ccccc4s3)c3[nH]ncc3c2)c2nc(N)ncc12
Structure:
Search PDB for entries with ligand similarity: