phorbol 12-myristate 13-acetate [Ligand Id: 2341] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL279115 (NSC-262244, Phorbol 12-myristate 13-acetate, Phorbol 12-myristate 13-acetate diester, Phorbol myristate acetate, Pma (phorbol ester), Tetradecanoylphorbol acetate, Tpa (phorbol ester))
  • Luciferin 4-monooxygenase in Photinus pyralis [ChEMBL: CHEMBL5567] [UniProtKB: P08659]
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  • 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 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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  • RAS guanyl releasing protein 3 in Human [ChEMBL: CHEMBL3638] [UniProtKB: Q8IV61]
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  • KNa1.1 in Rat [GtoPdb: 385] [UniProtKB: Q9Z258]
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  • KNa1.2 in Human [GtoPdb: 386] [UniProtKB: Q6UVM3]
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  • TRPV4 in Human [GtoPdb: 510] [UniProtKB: Q9HBA0]
  • TRPV4 in Mouse [GtoPdb: 510] [UniProtKB: Q9EPK8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Luciferin 4-monooxygenase in Photinus pyralis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5567] [UniProtKB: P08659]
ChEMBL Activation of firefly luciferase activity expressed in HEK293T cells after 6 hrs by luminescence assay B 8 pEC50 10 nM EC50 Bioorg Med Chem Lett (2019) 29: 585-590 [PMID:30600206]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5.2 pIC50 6309.57 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5.2 pIC50 6309.57 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
protein kinase C alpha/Protein kinase C alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
ChEMBL Displacement of [3H]PDBu from human recombinant PKCalpha after 20 mins by liquid scintillation counting B 8.19 pKi 6.4 nM Ki Bioorg Med Chem Lett (2011) 21: 3587-3590 [PMID:21596562]
ChEMBL Inhibition of [3H]-phorbol 12,13-dibutyrate (PDBu) binding to human recombinant protein kinase C alpha B 8.6 pKi 2.5 nM Ki Bioorg Med Chem Lett (2001) 11: 955-959 [PMID:11327599]
protein kinase C beta/Protein kinase C beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
ChEMBL Inhibition of [3H]-phorbol 12,13-dibutyrate (PDBu) binding to human recombinant protein kinase C beta B 8.74 pKi 1.8 nM Ki Bioorg Med Chem Lett (2001) 11: 955-959 [PMID:11327599]
protein kinase C delta/Protein kinase C delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2996] [GtoPdb: 1485] [UniProtKB: Q05655]
ChEMBL Inhibition of [3H]-phorbol 12,13-dibutyrate (PDBu) binding to human recombinant protein kinase C delta B 9.1 pKi 0.8 nM Ki Bioorg Med Chem Lett (2001) 11: 955-959 [PMID:11327599]
ChEMBL Binding affinity to GST-tagged PKCdelta expressed in Escherichia coli BL21(DE3) by fluorescence quenching B 5.29 pEC50 5170 nM EC50 Bioorg Med Chem (2010) 18: 1591-1598 [PMID:20100661]
ChEMBL Activation of PKCdelta (unknown origin) expressed in HEK293 cells harboring GFP-tagged RasGRP3 assessed as phosphorylation at ser299 residues after 30 mins by immunoblot method B 6.54 pEC50 290 nM EC50 J Med Chem (2018) 61: 6261-6276 [PMID:29860841]
protein kinase C epsilon/Protein kinase C epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3582] [GtoPdb: 1486] [UniProtKB: Q02156]
ChEMBL Inhibition of [3H]-phorbol 12,13-dibutyrate (PDBu) binding to human recombinant protein kinase C epsilon B 9.35 pKi 0.45 nM Ki Bioorg Med Chem Lett (2001) 11: 955-959 [PMID:11327599]
ChEMBL Binding affinity to GST-tagged PKCepsilon expressed in Escherichia coli BL21(DE3) by fluorescence quenching B 5.25 pEC50 5560 nM EC50 Bioorg Med Chem (2010) 18: 1591-1598 [PMID:20100661]
protein kinase C gamma/Protein kinase C gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2938] [GtoPdb: 1484] [UniProtKB: P05129]
ChEMBL Inhibition of [3H]-phorbol 12,13-dibutyrate (PDBu) binding to human recombinant protein kinase C gamma B 8.31 pKi 4.9 nM Ki Bioorg Med Chem Lett (2001) 11: 955-959 [PMID:11327599]
protein kinase C theta/Protein kinase C theta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759]
ChEMBL Binding affinity to GST-tagged PKCtheta expressed in Escherichia coli BL21(DE3) by fluorescence quenching B 5.5 pEC50 3190 nM EC50 Bioorg Med Chem (2010) 18: 1591-1598 [PMID:20100661]
RAS guanyl releasing protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3638] [UniProtKB: Q8IV61]
ChEMBL Activation of GFP-tagged RasGRP3 (unknown origin) expressed in HEK293 cells after 30 mins by immunoblot method B 7.09 pEC50 82 nM EC50 J Med Chem (2018) 61: 6261-6276 [PMID:29860841]
KNa1.1 in Rat [GtoPdb: 385] [UniProtKB: Q9Z258]
GtoPdb - - 7.3 pEC50 - - - J Neurosci (2006) 26: 5059-68 [PMID:16687497]
KNa1.2 in Human [GtoPdb: 386] [UniProtKB: Q6UVM3]
GtoPdb - - 7.92 pIC50 - - - J Neurosci (2006) 26: 5059-68 [PMID:16687497]
TRPV4 in Human [GtoPdb: 510] [UniProtKB: Q9HBA0]
GtoPdb - - 7.9 pEC50 12.5 nM EC50 Br J Pharmacol (2003) 140: 413-21 [PMID:12970074]
TRPV4 in Mouse [GtoPdb: 510] [UniProtKB: Q9EPK8]
GtoPdb - - 5.5 pEC50 - - - J Biol Chem (2002) 277: 13569-77 [PMID:11827975]

ChEMBL data shown on this page come from version 32:

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]