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Target
MAP kinase-activated protein kinase 2
Ligand
BDBM50344730
Substrate
n/a
Meas. Tech.
ChEMBL_749048 (CHEMBL1780645)
EC50
1.7±n/a nM
Citation
Kaptein, A; Oubrie, A; de Zwart, E; Hoogenboom, N; de Wit, J; van de Kar, B; van Hoek, M; Vogel, G; de Kimpe, V; Schultz-Fademrecht, C; Borsboom, J; van Zeeland, M; Versteegh, J; Kazemier, B; de Roos, J; Wijnands, F; Dulos, J; Jaeger, M; Leandro-Garcia, P; Barf, T Discovery of selective and orally available spiro-3-piperidyl ATP-competitive MK2 inhibitors. Bioorg Med Chem Lett 21:3823-7 (2011) [PubMed] Article
More Info.:
Target
Name:
MAP kinase-activated protein kinase 2
Synonyms:
MAP kinase-activated protein kinase 2 (MAPKAPK2) | MAP kinase-activated protein kinase 2 (MK2) | MAP kinase-activated protein kinase 2 (p38/MK2) | MAPK-Activated Protein Kinase 2 (MK2) | MAPK-activated protein kinase 2 | MAPK2_HUMAN | MAPKAP kinase 2 | MAPKAPK-2 | MAPKAPK2 | MK2
Type:
Serine/threonine-protein kinase
Mol. Mass.:
45579.87
Organism:
Homo sapiens (Human)
Description:
P49137
Residue:
400
Sequence:
MLSNSQGQSPPVPFPAPAPPPQPPTPALPHPPAQPPPPPPQQFPQFHVKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSHNSLTTPCYTPYYVAPEVLGPEKYDKSCDMWSLGVIMYILLCGYPPFYSNHGLAISPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLKEDKERWEDVKEEMTSALATMRVDYEQIKIKKIEDASNPLLLKRRKKARALEAAALAH
Inhibitor
Name:
BDBM50344730
Synonyms:
2'-(2'-(cyclopentylamino)-2,5'-bipyrimidin-4-yl)-5',6'-dihydrospiro[piperidine-4,7'-pyrrolo[3,2-c]pyridin]-4'(1'H)-one | CHEMBL1779367
Type:
Small organic molecule
Emp. Form.:
C24H28N8O
Mol. Mass.:
444.5321
SMILES:
O=C1NCC2(CCNCC2)c2[nH]c(cc12)-c1ccnc(n1)-c1cnc(NC2CCCC2)nc1