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Target
MAP kinase-activated protein kinase 3
Ligand
BDBM50583520
Substrate
n/a
Meas. Tech.
ChEMBL_2157589 (CHEMBL5042249)
IC50
>5000±n/a nM
Citation
 M Serafim, RA; da Silva Santiago, A; Schwalm, MP; Hu, Z; Dos Reis, CV; Takarada, JE; Mezzomo, P; Massirer, KB; Kudolo, M; Gerstenecker, S; Chaikuad, A; Zender, L; Knapp, S; Laufer, S; Couņago, RM; Gehringer, M Development of the First Covalent Monopolar Spindle Kinase 1 (MPS1/TTK) Inhibitor. J Med Chem 65:3173-3192 (2022) [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:
BDBM50583520
Synonyms:
CHEMBL5094006
Type:
Small organic molecule
Emp. Form.:
C35H40N8O2
Mol. Mass.:
604.7445
SMILES:
CCc1cccc(CC)c1NC(=O)c1ccn-2c1CCc1cnc(Nc3ccc(cc3NC(=O)C=C)N3CCN(C)CC3)nc-21
Structure:
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