Target
Mitogen-activated protein kinase 8
Ligand
BDBM26057
Substrate
n/a
Meas. Tech.
ChEMBL_612736 (CHEMBL1070200)
IC50
280±n/a nM
Citation
 De, SKChen, VStebbins, JLChen, LHCellitti, JFMachleidt, TBarile, ERiel-Mehan, MDahl, RYang, LEmdadi, AMurphy, RPellecchia, M Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors. Bioorg Med Chem 18:590-6 (2010) [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:
BDBM26057
Synonyms:
4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-4H-1,2,4-triazol-3-ol | BI-78D3
Type:
Small organic molecule
Emp. Form.:
C13H9N5O5S2
Mol. Mass.:
379.371
SMILES:
[O-][N+](=O)c1cnc(Sc2n[nH]c(=O)n2-c2ccc3OCCOc3c2)s1
Structure:
Search PDB for entries with ligand similarity: