Reaction Details
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Mitogen-activated protein kinase 8
Ligand
BDBM86627
Substrate
n/a
Meas. Tech.
JNK Kinase Assay
IC50
809±0.0 nM
Citation
Zhang, T; Inesta-Vaquera, F; Niepel, M; Zhang, J; Ficarro, SB; Machleidt, T; Xie, T; Marto, JA; Kim, N; Sim, T; Laughlin, JD; Park, H; LoGrasso, PV; Patricelli, M; Nomanbhoy, TK; Sorger, PK; Alessi, DR; Gray, NS Discovery of potent and selective covalent inhibitors of JNK. Chem Biol 19:140-54 (2012) [PubMed] Article More Info.:
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:
BDBM86627
Synonyms:
JNK-IN-2
Type:
Small organic molecule
Emp. Form.:
C28H27N7O2
Mol. Mass.:
493.5597
SMILES:
CN(C)C\C=C\C(=O)Nc1ccc(cc1)C(=O)Nc1cccc(Nc2nccc(n2)-c2cccnc2)c1
Structure:
