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Target
Mitogen-activated protein kinase 8
Ligand
BDBM50296636
Substrate
n/a
Meas. Tech.
ChEMBL_582357 (CHEMBL1063394)
IC50
>10000±n/a nM
Citation
Wurz, RP; Pettus, LH; Xu, S; Henkle, B; Sherman, L; Plant, M; Miner, K; McBride, H; Wong, LM; Saris, CJ; Lee, MR; Chmait, S; Mohr, C; Hsieh, F; Tasker, AS Part 1: Structure-Activity Relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase. Bioorg Med Chem Lett 19:4724-8 (2009) [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:
BDBM50296636
Synonyms:
4-chloro-N-cyclopropyl-3-(1-(4-fluorophenyl)-7-methyl-6-oxo-6,7-dihydro-1H-pyrazolo[3,4-b]pyridin-4-ylamino)benzamide | CHEMBL561932
Type:
Small organic molecule
Emp. Form.:
C23H19ClFN5O2
Mol. Mass.:
451.881
SMILES:
Cn1c2n(ncc2c(Nc2cc(ccc2Cl)C(=O)NC2CC2)cc1=O)-c1ccc(F)cc1