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Target
Mitogen-activated protein kinase 8
Ligand
BDBM32460
Substrate
biotinylated-ATF2
Meas. Tech.
Homogeneous Time-resolved Fluorescence Assay
IC50
140±n/a nM
Citation
 Shin, Y; Chen, W; Habel, J; Duckett, D; Ling, YY; Koenig, M; He, Y; Vojkovsky, T; LoGrasso, P; Kamenecka, TM Synthesis and SAR of piperazine amides as novel c-jun N-terminal kinase (JNK) inhibitors. Bioorg Med Chem Lett 19:3344-7 (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:
BDBM32460
Synonyms:
piperazine amide, 4g
Type:
Small organic molecule
Emp. Form.:
C18H17BrClN3O2
Mol. Mass.:
422.703
SMILES:
Clc1cccc(NC(=O)c2ccc(Br)o2)c1N1CCN(CC#C)CC1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
biotinylated-ATF2
Synonyms:
Activating transcription factor 2 | Cyclic AMP-dependent transcription factor ATF-2 | cAMP response element-binding protein CRE-BP1
Type:
Other Protein Type
Mol. Mass.:
13150.37
Organism:
Homo sapiens (Human)
Description:
ATF-2 (aa 1-115) was expressed and purified from E. coli.
Residue:
115
Sequence:
MKFKLHVNSARQYKDLWNMSDDKPFLCTAPGCGQRFTNEDHLAVHKHKHEMTLKFGPARNDSVIVADQTPTPTRFLKNCEEVGLFNELASPFENEFKKASEDDIKKMPLDLSPLA