Reaction Details Report a problem with these data
Target
MAP kinase-activated protein kinase 3
Ligand
BDBM50220232
Substrate
n/a
Meas. Tech.
ChEMBL_449183 (CHEMBL899448)
IC50
4520±n/a nM
Citation
Hamblett, CL; Methot, JL; Mampreian, DM; Sloman, DL; Stanton, MG; Kral, AM; Fleming, JC; Cruz, JC; Chenard, M; Ozerova, N; Hitz, AM; Wang, H; Deshmukh, SV; Nazef, N; Harsch, A; Hughes, B; Dahlberg, WK; Szewczak, AA; Middleton, RE; Mosley, RT; Secrist, JP; Miller, TA The discovery of 6-amino nicotinamides as potent and selective histone deacetylase inhibitors. Bioorg Med Chem Lett 17:5300-9 (2007) [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:
BDBM50220232
Synonyms:
(S)-benzyl 4-(5-((2-aminophenyl)carbamoyl)pyridin-2-yl)-2-methylpiperazine-1-carboxylate | (S)-benzyl 4-(5-(2-aminophenylcarbamoyl)pyridin-2-yl)-2-methylpiperazine-1-carboxylate | CHEMBL236902
Type:
Small organic molecule
Emp. Form.:
C25H27N5O3
Mol. Mass.:
445.5136
SMILES:
C[C@H]1CN(CCN1C(=O)OCc1ccccc1)c1ccc(cn1)C(=O)Nc1ccccc1N |r|