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Target
Mitogen-activated protein kinase 8
Ligand
BDBM50341372
Substrate
n/a
Meas. Tech.
ChEMBL_1544314 (CHEMBL3751431)
IC50
4220±n/a nM
Citation
 Simon-Szabó, L; Kokas, M; Greff, Z; Boros, S; Bánhegyi, P; Zsákai, L; Szántai-Kis, C; Vantus, T; Mandl, J; Bánhegyi, G; Vályi-Nagy, I; Orfi, L; Ullrich, A; Csala, M; Kéri, G Novel compounds reducing IRS-1 serine phosphorylation for treatment of diabetes. Bioorg Med Chem Lett 26:424-8 (2016) [PubMed]  Article
Target
Name:
Mitogen-activated protein kinase 8
Synonyms:
JNK-46 | JNK1 | JNK1-alpha-1 | MAPK8 | MK08_HUMAN | Mitogen-Activated Protein Kinase 8 (JNK1) | PRKM8 | SAPK1 | SAPK1C | Stress-activated protein kinase JNK1 | c-Jun N-terminal kinase 1 | c-Jun N-terminal kinase 1 (JNK1) | c-Jun N-terminal kinase 1(JNK1) | c-Jun N-terminal kinase 2 (JNK2)
Type:
Enzyme
Mol. Mass.:
48297.57
Organism:
Homo sapiens (Human)
Description:
JNK-1 was purchased from Upstate Cell Signaling Solutions (formerly Upstate Biotechnology).
Residue:
427
Sequence:
MSRSKRDNNFYSVEIGDSTFTVLKRYQNLKPIGSGAQGIVCAAYDAILERNVAIKKLSRPFQNQTHAKRAYRELVLMKCVNHKNIIGLLNVFTPQKSLEEFQDVYIVMELMDANLCQVIQMELDHERMSYLLYQMLCGIKHLHSAGIIHRDLKPSNIVVKSDCTLKILDFGLARTAGTSFMMTPYVVTRYYRAPEVILGMGYKENVDLWSVGCIMGEMVCHKILFPGRDYIDQWNKVIEQLGTPCPEFMKKLQPTVRTYVENRPKYAGYSFEKLFPDVLFPADSEHNKLKASQARDLLSKMLVIDASKRISVDEALQHPYINVWYDPSEAEAPPPKIPDKQLDEREHTIEEWKELIYKEVMDLEERTKNGVIRGQPSPLGAAVINGSQHPSSSSSVNDVSSMSTDPTLASDTDSSLEAAAGPLGCCR
  
Inhibitor
Name:
BDBM50341372
Synonyms:
6-(2,4-Difluorophenoxy)-2-isopropylamino-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one | 6-(2,4-difluorophenoxy)-8-methyl-2-[(1-methylethyl)amino]pyrido[2,3-d]pyrimidin-7(8H)-one | CHEMBL1232772
Type:
Small organic molecule
Emp. Form.:
C17H16F2N4O2
Mol. Mass.:
346.3313
SMILES:
CC(C)Nc1ncc2cc(Oc3ccc(F)cc3F)c(=O)n(C)c2n1
Structure:
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