Target
Mitogen-activated protein kinase 8
Ligand
BDBM50253152
Substrate
n/a
Meas. Tech.
ChEMBL_539861 (CHEMBL1025669)
IC50
>10000±n/a nM
Citation
 Herberich, BCao, GQChakrabarti, PPFalsey, JRPettus, LRzasa, RMReed, ABReichelt, ASham, KThaman, MWurz, RPXu, SZhang, DHsieh, FLee, MRSyed, RLi, VGrosfeld, DPlant, MHHenkle, BSherman, LMiddleton, SWong, LMTasker, AS Discovery of highly selective and potent p38 inhibitors based on a phthalazine scaffold. J Med Chem 51:6271-9 (2008) [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:
Human
Description:
JNK-1 was purchased from Upstate Cell Signaling Solutions (formerly Upstate Biotechnology).
Residue:
427
Sequence:
MSRSKRDNNFYSVEIGDSTFTVLKRYQNLKPIGSGAQGIVCAAYDAILERNVAIKKLSRPFQNQTHAKRAYRELVLMKCVNHKNIIGLLNVFTPQKSLEEFQDVYIVMELMDANLCQVIQMELDHERMSYLLYQMLCGIKHLHSAGIIHRDLKPSNIVVKSDCTLKILDFGLARTAGTSFMMTPYVVTRYYRAPEVILGMGYKENVDLWSVGCIMGEMVCHKILFPGRDYIDQWNKVIEQLGTPCPEFMKKLQPTVRTYVENRPKYAGYSFEKLFPDVLFPADSEHNKLKASQARDLLSKMLVIDASKRISVDEALQHPYINVWYDPSEAEAPPPKIPDKQLDEREHTIEEWKELIYKEVMDLEERTKNGVIRGQPSPLGAAVINGSQHPSSSSSVNDVSSMSTDPTLASDTDSSLEAAAGPLGCCR
  
Inhibitor
Name:
BDBM50253152
Synonyms:
CHEMBL493708 | N-Cyclopropyl-4-methyl-3-(1-((R)-2,2,2-trifluoro-1-methylethoxy)-6-phthalazinyl)benzamide
Type:
Small organic molecule
Emp. Form.:
C22H20F3N3O2
Mol. Mass.:
415.4083
SMILES:
C[C@@H](Oc1nncc2cc(ccc12)-c1cc(ccc1C)C(=O)NC1CC1)C(F)(F)F |r|
Structure:
Search PDB for entries with ligand similarity: