Target
Mitogen-activated protein kinase 8
Ligand
BDBM29300
Substrate
Biotin-labeled pepJIP1
Meas. Tech.
DELFIA Assay (Dissociation Enhanced Lanthanide Fluoro-Immuno Assay)
pH
7.8±n/a
Temperature
273.15±n/a K
IC50
45±n/a nM
Citation
 De, SKStebbins, JLChen, LHRiel-Mehan, MMachleidt, TDahl, RYuan, HEmdadi, ABarile, EChen, VMurphy, RPellecchia, M Design, synthesis, and structure-activity relationship of substrate competitive, selective, and in vivo active triazole and thiadiazole inhibitors of the c-Jun N-terminal kinase. J Med Chem 52:1943-52 (2009) [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:
BDBM29300
Synonyms:
triazole, 3r
Type:
Small organic molecule
Emp. Form.:
C12H9N5O4S2
Mol. Mass.:
351.361
SMILES:
COc1ccc(cc1)-n1c(Sc2ncc(s2)[N+]([O-])=O)n[nH]c1=O
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Biotin-labeled pepJIP1
Synonyms:
biotinylated peptide derived from JNK-interacting protein 1.
Type:
Peptide
Mol. Mass.:
2132.62
Organism:
n/a
Description:
lc indicates a hydrocarbon chain of six methylene groups was added.
Residue:
18
Sequence:
ITINLCKRPKRPTTLNLF