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Target
MAP kinase-activated protein kinase 3
Ligand
BDBM50224883
Substrate
n/a
Meas. Tech.
ChEMBL_458463 (CHEMBL941780)
Ki
>9234±n/a nM
Citation
 Tao, ZF; Chen, Z; Bui, MH; Kovar, P; Johnson, E; Bouska, J; Zhang, H; Rosenberg, S; Sowin, T; Lin, NH Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics. Bioorg Med Chem Lett 17:6593-601 (2007) [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:
BDBM50224883
Synonyms:
7-chloro-3-oxo-8-[(thiazol-5-ylmethyl)-amino]-11,16-dioxa-2,4,19,21-tetraaza-tricyclo[15.3.1.0*5,10*]henicosa-1(21),5,7,9,17,19-hexaene-18-crbonitrile | CHEMBL248757
Type:
Small organic molecule
Emp. Form.:
C20H18ClN7O3S
Mol. Mass.:
471.92
SMILES:
Clc1cc2NC(=O)Nc3cnc(C#N)c(OCCCCOc2cc1NCc1cncs1)n3
Structure:
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