JNK inhibitor V [Ligand Id: 5997] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL191384 (AS-601245)
  • mitogen-activated protein kinase 8/c-Jun N-terminal kinase 1 in Human [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983]
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  • mitogen-activated protein kinase 9/c-Jun N-terminal kinase 2 in Human [ChEMBL: CHEMBL4179] [GtoPdb: 1497] [UniProtKB: P45984]
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  • mitogen-activated protein kinase 10/c-Jun N-terminal kinase 3 in Human [ChEMBL: CHEMBL2637] [GtoPdb: 1498] [UniProtKB: P53779]
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  • dual specificity tyrosine phosphorylation regulated kinase 2/Dual-specificity tyrosine-phosphorylation regulated kinase 2 in Human [ChEMBL: CHEMBL4376] [GtoPdb: 2011] [UniProtKB: Q92630]
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  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
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  • eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
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  • Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
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  • Pim-3 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM3 in Human [ChEMBL: CHEMBL5407] [GtoPdb: 2160] [UniProtKB: Q86V86]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mitogen-activated protein kinase 8/c-Jun N-terminal kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983]
ChEMBL Inhibition of JNK1 in the presence of 20uM ATP B 5.59 pIC50 2600 nM IC50 Biochem J (2007) 408: 297-315 [PMID:17850214]
ChEMBL Inhibition of human JNK1 B 6.82 pIC50 150 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of human JNK1 by radiometric assay B 6.82 pIC50 150 nM IC50 Bioorg Med Chem (2008) 16: 4715-4732 [PMID:18313304]
ChEMBL Inhibition of JNK1 B 6.82 pIC50 150 nM IC50 J Med Chem (2010) 53: 3005-3012 [PMID:20146479]
mitogen-activated protein kinase 9/c-Jun N-terminal kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4179] [GtoPdb: 1497] [UniProtKB: P45984]
ChEMBL Inhibition of JNK2 in the presence of 20uM ATP B 5.3 pIC50 5000 nM IC50 Biochem J (2007) 408: 297-315 [PMID:17850214]
ChEMBL Inhibition of human JNK2 B 6.66 pIC50 220 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of JNK2 B 6.66 pIC50 220 nM IC50 J Med Chem (2010) 53: 3005-3012 [PMID:20146479]
mitogen-activated protein kinase 10/c-Jun N-terminal kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2637] [GtoPdb: 1498] [UniProtKB: P53779]
ChEMBL Inhibition of JNK3 B 6.92 pIC50 120 nM IC50 J Med Chem (2010) 53: 419-431 [PMID:19947601]
GtoPdb - - 7.15 pIC50 70 nM IC50
ChEMBL Inhibition of JNK3 B 7.15 pIC50 70 nM IC50 Bioorg Med Chem (2007) 15: 4256-4264 [PMID:17451961]
ChEMBL Inhibition of human JNK3 B 7.15 pIC50 70 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of JNK3 B 7.15 pIC50 70 nM IC50 J Med Chem (2010) 53: 3005-3012 [PMID:20146479]
dual specificity tyrosine phosphorylation regulated kinase 2/Dual-specificity tyrosine-phosphorylation regulated kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4376] [GtoPdb: 2011] [UniProtKB: Q92630]
ChEMBL Inhibition of DYRK2 in the presence of 50uM ATP B 6.52 pIC50 300 nM IC50 Biochem J (2007) 408: 297-315 [PMID:17850214]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
ChEMBL Inhibition of GSK3-beta in the presence of 20uM ATP B 7.4 pIC50 40 nM IC50 Biochem J (2007) 408: 297-315 [PMID:17850214]
eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
ChEMBL Inhibition of human recombinant PKR autophosphorylation using poly[I:C] after 10 mins by luminescent assay B 7 pIC50 <100 nM IC50 Bioorg Med Chem Lett (2011) 21: 4108-4114 [PMID:21632247]
Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
ChEMBL Inhibition of PIM1 in the presence of 20uM ATP B 7.1 pIC50 80 nM IC50 Biochem J (2007) 408: 297-315 [PMID:17850214]
Pim-3 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5407] [GtoPdb: 2160] [UniProtKB: Q86V86]
ChEMBL Inhibition of PIM3 in the presence of 5uM ATP B 7.52 pIC50 30 nM IC50 Biochem J (2007) 408: 297-315 [PMID:17850214]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]