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

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ChEMBL ligand: CHEMBL1863513 (AGN 204332, AGN204332, 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 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]