Target
Mitogen-activated protein kinase 8
Ligand
BDBM50334006
Substrate
n/a
Meas. Tech.
ChEMBL_701207 (CHEMBL1648827)
IC50
1700±n/a nM
Citation
 Probst, GDBowers, SSealy, JMTruong, APHom, RKGalemmo, RAKonradi, AWSham, HLQuincy, DAPan, HYao, NLin, MTóth, GArtis, DRZmolek, WWong, KQin, ALorentzen, CNakamura, DFQuinn, KPSauer, JMPowell, KRuslim, LWright, SChereau, DRen, ZAnderson, JPBard, FYednock, TAGriswold-Prenner, I Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration. Bioorg Med Chem Lett 21:315-9 (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:
BDBM50334006
Synonyms:
4-(6-aminonaphthalen-2-yl)-3-(2-(tetrahydro-2H-pyran-4-ylamino)pyridin-4-yl)-1H-1,2,4-triazol-5(4H)-one | CHEMBL1644633
Type:
Small organic molecule
Emp. Form.:
C22H22N6O2
Mol. Mass.:
402.4491
SMILES:
Nc1ccc2cc(ccc2c1)-n1c(n[nH]c1=O)-c1ccnc(NC2CCOCC2)c1
Structure:
Search PDB for entries with ligand similarity: