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

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ChEMBL ligand: CHEMBL1863513 (AGN 204332, Ingenol mebutate, PEP-005, PEP005, Picato)
  • 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 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]