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)) |
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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 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]
