10-Me-Aplog-1 [Ligand Id: 13409] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2148108
  • 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 delta/Protein kinase C delta in Human [ChEMBL: CHEMBL2996] [GtoPdb: 1485] [UniProtKB: Q05655]
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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 eta/Protein kinase C eta in Human [ChEMBL: CHEMBL3616] [GtoPdb: 1487] [UniProtKB: P24723]
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  • protein kinase C gamma/Protein kinase C gamma in Human [ChEMBL: CHEMBL2938] [GtoPdb: 1484] [UniProtKB: P05129]
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  • protein kinase C theta/Protein kinase C theta in Human [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759]
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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 Inhibition of [3H]PDBu binding to PKCalpha C1A domain B 8.33 pKi 4.7 nM Ki J Med Chem (2012) 55: 5614-5626 [PMID:22625994]
GtoPdb Binding affinity for the C1A domain of PKCα, determined by inhibition of [3H]PDBu binding - 8.33 pKi 4.7 nM Ki J Med Chem (2012) 55: 5614-26 [PMID:22625994]
protein kinase C beta/Protein kinase C beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
GtoPdb Binding affinity for the C1A domain of PKCβ, determined by inhibition of [3H]PDBu binding - 7.92 pKi 12 nM Ki J Med Chem (2012) 55: 5614-26 [PMID:22625994]
ChEMBL Inhibition of [3H]PDBu binding to PKCbeta C1A domain B 7.92 pKi 12 nM Ki J Med Chem (2012) 55: 5614-5626 [PMID:22625994]
protein kinase C delta/Protein kinase C delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2996] [GtoPdb: 1485] [UniProtKB: Q05655]
ChEMBL Inhibition of [3H]PDBu binding to PKCdelta-C1A domain peptide (unknown origin) B 7.66 pKi 22 nM Ki Bioorg Med Chem (2013) 21: 2695-2702 [PMID:23582444]
ChEMBL Inhibition of [3H]PDBu binding to PKCdelta C1B domain B 9.34 pKi 0.46 nM Ki J Med Chem (2012) 55: 5614-5626 [PMID:22625994]
GtoPdb Binding affinity for the C1B domain of PKCδ, determined by inhibition of [3H]PDBu binding - 9.34 pKi 0.46 nM Ki J Med Chem (2012) 55: 5614-26 [PMID:22625994]
protein kinase C epsilon/Protein kinase C epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3582] [GtoPdb: 1486] [UniProtKB: Q02156]
ChEMBL Inhibition of [3H]PDBu binding to PKCepsilon C1B domain B 8.7 pKi 2 nM Ki J Med Chem (2012) 55: 5614-5626 [PMID:22625994]
GtoPdb Binding affinity for the C1B domain of PKCε, determined by inhibition of [3H]PDBu binding - 8.7 pKi 2 nM Ki J Med Chem (2012) 55: 5614-26 [PMID:22625994]
protein kinase C eta/Protein kinase C eta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3616] [GtoPdb: 1487] [UniProtKB: P24723]
ChEMBL Inhibition of [3H]PDBu binding to PKCeta C1B domain B 9.35 pKi 0.45 nM Ki J Med Chem (2012) 55: 5614-5626 [PMID:22625994]
GtoPdb Binding affinity for the C1B domain of PKCη, determined by inhibition of [3H]PDBu binding - 9.35 pKi 0.45 nM Ki J Med Chem (2012) 55: 5614-26 [PMID:22625994]
protein kinase C gamma/Protein kinase C gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2938] [GtoPdb: 1484] [UniProtKB: P05129]
ChEMBL Inhibition of [3H]PDBu binding to PKCgamma C1A domain B 8.26 pKi 5.5 nM Ki J Med Chem (2012) 55: 5614-5626 [PMID:22625994]
GtoPdb Binding affinity for the C1A domain of PKCγ, determined by inhibition of [3H]PDBu binding - 8.26 pKi 5.5 nM Ki J Med Chem (2012) 55: 5614-26 [PMID:22625994]
protein kinase C theta/Protein kinase C theta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759]
ChEMBL Inhibition of [3H]PDBu binding to PKCtheta C1B domain B 9.27 pKi 0.54 nM Ki J Med Chem (2012) 55: 5614-5626 [PMID:22625994]
GtoPdb Binding affinity for the C1B domain of PKCθ, determined by inhibition of [3H]PDBu binding - 9.27 pKi 0.54 nM Ki J Med Chem (2012) 55: 5614-26 [PMID:22625994]

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]