PKCbeta inhibitor [Ligand Id: 6025] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL366266
  • protein kinase C alpha/Protein kinase C alpha in Human [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
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  • protein kinase C beta/Protein kinase C beta in Human [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
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  • protein kinase C epsilon/Protein kinase C epsilon in Human [ChEMBL: CHEMBL3582] [GtoPdb: 1486] [UniProtKB: Q02156]
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  • protein kinase C gamma/Protein kinase C gamma in Human [ChEMBL: CHEMBL2938] [GtoPdb: 1484] [UniProtKB: P05129]
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  • Janus kinase 1/Tyrosine-protein kinase JAK1 in Human [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
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  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
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  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
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  • tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
protein kinase C alpha/Protein kinase C alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
ChEMBL Inhibitory concentration against recombinant human Protein kinase C alpha B 6.48 pIC50 331 nM IC50 Bioorg Med Chem Lett (2004) 14: 5171-5174 [PMID:15380221]
ChEMBL Inhibition of PKCalpha B 6.48 pIC50 331 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
protein kinase C beta/Protein kinase C beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
ChEMBL Inhibitory concentration against recombinant human Protein kinase C beta 1 B 7.68 pIC50 21 nM IC50 Bioorg Med Chem Lett (2004) 14: 5171-5174 [PMID:15380221]
ChEMBL Inhibition of PKCbeta2 (unknown origin) B 8.3 pIC50 5.01 nM IC50 Med Chem Res (2011) 20: 1188-1199
GtoPdb - - 8.3 pIC50 5 nM IC50 Bioorg Med Chem Lett (2004) 14: 5171-4 [PMID:15380221]
ChEMBL Inhibitory concentration against recombinant human Protein kinase C beta 2 B 8.3 pIC50 5 nM IC50 Bioorg Med Chem Lett (2004) 14: 5171-5174 [PMID:15380221]
ChEMBL Inhibition of PKCbeta B 8.3 pIC50 5 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of PKCbeta2 (unknown origin) B 8.3 pIC50 5 nM IC50 Med Chem Res (2011) 20: 1188-1199
protein kinase C epsilon/Protein kinase C epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3582] [GtoPdb: 1486] [UniProtKB: Q02156]
ChEMBL Inhibitory concentration against recombinant human Protein kinase C epsilon B 5.55 pIC50 2807 nM IC50 Bioorg Med Chem Lett (2004) 14: 5171-5174 [PMID:15380221]
ChEMBL Inhibition of PKCepsilon B 5.55 pIC50 2800 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
protein kinase C gamma/Protein kinase C gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2938] [GtoPdb: 1484] [UniProtKB: P05129]
ChEMBL Inhibition of PKCgamma B 6 pIC50 >1000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
ChEMBL Inhibition of JAK1 (unknown origin) B 6.11 pIC50 770 nM IC50 Bioorg Med Chem Lett (2014) 24: 1116-1121 [PMID:24461299]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL Inhibition of JAK2 (unknown origin) B 5.41 pIC50 3850 nM IC50 Bioorg Med Chem Lett (2014) 24: 1116-1121 [PMID:24461299]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
ChEMBL Inhibition of JAK3 (unknown origin) B 7.77 pIC50 17 nM IC50 Bioorg Med Chem Lett (2014) 24: 1116-1121 [PMID:24461299]
tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
ChEMBL Inhibition of TYK2 (unknown origin) B 5.64 pIC50 2310 nM IC50 Bioorg Med Chem Lett (2014) 24: 1116-1121 [PMID:24461299]

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]