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Target
Mitogen-activated protein kinase 8
Ligand
BDBM15917
Substrate
biotinylated GST-ATF2
Meas. Tech.
ATF-2 Phosphorylation Assay
pH
7.2±n/a
Temperature
293.15±n/a K
IC50
6400±n/a nM
Citation
Zhao, H; Serby, MD; Xin, Z; Szczepankiewicz, BG; Liu, M; Kosogof, C; Liu, B; Nelson, LT; Johnson, EF; Wang, S; Pederson, T; Gum, RJ; Clampit, JE; Haasch, DL; Abad-Zapatero, C; Fry, EH; Rondinone, C; Trevillyan, JM; Sham, HL; Liu, G Discovery of potent, highly selective, and orally bioavailable pyridine carboxamide c-Jun NH2-terminal kinase inhibitors. J Med Chem 49:4455-8 (2006) [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:
BDBM15917
Synonyms:
2-pyridinecarboxamide deriv. 8g | 4-amino-5-cyano-6-ethoxy-N-[(4-methanesulfonylphenyl)methyl]-N-methylpyridine-2-carboxamide
Type:
Small organic molecule
Emp. Form.:
C18H20N4O4S
Mol. Mass.:
388.441
SMILES:
CCOc1nc(cc(N)c1C#N)C(=O)N(C)Cc1ccc(cc1)S(C)(=O)=O
Substrate
Name:
biotinylated GST-ATF2
Synonyms:
ATF-2-GST | ATF2 | Activating transcription factor 2 | Activating transcription factor 2-GST fusion | GST-ATF2 | biotinylated ATF2 substrate | biotinylated activating transcription factor 2
Type:
Other Protein Type
Mol. Mass.:
12237.77
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
109
Sequence:
MSDDKPFLCTAPGCGQRFTNEDHLAVHKHKHEMTLKFGPARNDSVIVADQTPTPTRFLKNCEEVGLFNELASPFENEFKKASEDDIKKMPLDLSPLATPIIRSKIEEPS