Reaction Details Report a problem with these data
Target
Mitogen-activated protein kinase 8
Ligand
BDBM50169959
Substrate
n/a
Meas. Tech.
JNK Kinase Assay
IC50
150±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:
Human
Description:
JNK-1 was purchased from Upstate Cell Signaling Solutions (formerly Upstate Biotechnology).
Residue:
427
Sequence:
MSRSKRDNNFYSVEIGDSTFTVLKRYQNLKPIGSGAQGIVCAAYDAILERNVAIKKLSRPFQNQTHAKRAYRELVLMKCVNHKNIIGLLNVFTPQKSLEEFQDVYIVMELMDANLCQVIQMELDHERMSYLLYQMLCGIKHLHSAGIIHRDLKPSNIVVKSDCTLKILDFGLARTAGTSFMMTPYVVTRYYRAPEVILGMGYKENVDLWSVGCIMGEMVCHKILFPGRDYIDQWNKVIEQLGTPCPEFMKKLQPTVRTYVENRPKYAGYSFEKLFPDVLFPADSEHNKLKASQARDLLSKMLVIDASKRISVDEALQHPYINVWYDPSEAEAPPPKIPDKQLDEREHTIEEWKELIYKEVMDLEERTKNGVIRGQPSPLGAAVINGSQHPSSSSSVNDVSSMSTDPTLASDTDSSLEAAAGPLGCCR
Inhibitor
Name:
BDBM50169959
Synonyms:
2-(benzo[d]thiazol-2(3H)-ylidene)-2-(2-(2-(pyridin-3-yl)ethylamino)pyrimidin-4-yl)acetonitrile | AS-601245 | AS601245 | CHEMBL1788116 | CHEMBL191384 | [3H-Benzothiazol-(2Z)-ylidene]-[2-(2-pyridin-3-yl-ethylamino)-pyrimidin-4-yl]-acetonitrile
Type:
Small organic molecule
Emp. Form.:
C20H16N6S
Mol. Mass.:
372.446
SMILES:
N#CC(c1nc2ccccc2s1)c1ccnc(NCCc2cccnc2)n1