ingenol mebutate [Ligand Id: 7443] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1863513 (Picato, Ingenol mebutate, AGN 204332, PEP-005, PEP005)
  • protein kinase C delta/Protein kinase C delta in Human [ChEMBL: CHEMBL2996] [GtoPdb: 1485] [UniProtKB: Q05655]
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  • protein kinase C alpha in Human [GtoPdb: 1482] [UniProtKB: P17252]
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  • protein kinase C beta in Human [GtoPdb: 1483] [UniProtKB: P05771]
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  • protein kinase C gamma in Human [GtoPdb: 1484] [UniProtKB: P05129]
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  • protein kinase C epsilon in Human [GtoPdb: 1486] [UniProtKB: Q02156]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
protein kinase C delta/Protein kinase C delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2996] [GtoPdb: 1485] [UniProtKB: Q05655]
GtoPdb - - 9.42 pKi 0.38 nM Ki Cancer Res (2004) 64: 3243-55 [PMID:15126366]
ChEMBL Activation of PKCdelta (unknown origin) using phosphatidylserine as substrate B 8.39 pEC50 4.1 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 5624-5629 [PMID:23993332]
ChEMBL Activation of PKCdelta (unknown origin) after 40 mins B 8.39 pEC50 4.1 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 54-60 [PMID:24332494]
protein kinase C alpha in Human [GtoPdb: 1482] [UniProtKB: P17252]
GtoPdb - - 9.52 pKi 0.3 nM Ki Cancer Res (2004) 64: 3243-55 [PMID:15126366]
protein kinase C beta in Human [GtoPdb: 1483] [UniProtKB: P05771]
GtoPdb - - 9.98 pKi 0.1 nM Ki Cancer Res (2004) 64: 3243-55 [PMID:15126366]
protein kinase C gamma in Human [GtoPdb: 1484] [UniProtKB: P05129]
GtoPdb - - 9.79 pKi 0.16 nM Ki Cancer Res (2004) 64: 3243-55 [PMID:15126366]
protein kinase C epsilon in Human [GtoPdb: 1486] [UniProtKB: Q02156]
GtoPdb - - 9.77 pKi 0.17 nM Ki Cancer Res (2004) 64: 3243-55 [PMID:15126366]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]