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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]