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 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]
