myristic acid [Ligand Id: 2806] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL111077 (FEMA NO. 2764, Myristate, Myristic acid, NSC-5028, N-tetradecan-1-oic acid, N-tetradecanoic acid, PHILACID-1400, PRIFRAC-2942)
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  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
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  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
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  • FFA4 receptor in Human [GtoPdb: 127] [UniProtKB: Q5NUL3]
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  • FFA1 receptor in Human [GtoPdb: 225] [UniProtKB: O14842]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Dynamin-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4958] [UniProtKB: Q05193]
ChEMBL Concentration required against dynamin-1 GTPase activity of sheep brain. B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (2004) 14: 3275-3278 [PMID:15149689]
GPR84/G-protein coupled receptor 84 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3714079] [GtoPdb: 120] [UniProtKB: Q9NQS5]
ChEMBL Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method B 5.58 pKi 2640 nM Ki J Med Chem (2020) 63: 2391-2410 [PMID:31721581]
ChEMBL Agonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting method F 4.84 pEC50 14400 nM EC50 J Med Chem (2020) 63: 15399-15409 [PMID:33267584]
ChEMBL Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay F 4.94 pEC50 11400 nM EC50 J Med Chem (2020) 63: 2391-2410 [PMID:31721581]
ChEMBL Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay B 5.15 pEC50 7010 nM EC50 J Med Chem (2020) 63: 2391-2410 [PMID:31721581]
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
ChEMBL Displacement of [3H]GW2331 from Homo sapiens (human) PPARalpha receptor by scintillation proximity assay B 5.27 pIC50 5400 nM IC50 Med Chem Res (2013) 22: 3126-3133
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
ChEMBL Displacement of [3H]GW2433 from Homo sapiens (human) PPARdelta receptor by scintillation proximity assay B 4.62 pIC50 24000 nM IC50 Med Chem Res (2013) 22: 3126-3133
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
ChEMBL Displacement of [3H]BRL49653 from Homo sapiens (human) PPARgamma receptor by scintillation proximity assay B 4.68 pIC50 21000 nM IC50 Med Chem Res (2013) 22: 3126-3133
TLR2/Toll-like receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4163] [GtoPdb: 1752] [UniProtKB: O60603]
ChEMBL Inhibition of TLR2 agonist Pam3Cys-Ser-(Lys)4-OH-mediated IL8 secretion in THP1 cells F 5.3 pIC50 5000 nM IC50 J Med Chem (2006) 49: 1754-1765 [PMID:16509590]
FFA4 receptor in Human [GtoPdb: 127] [UniProtKB: Q5NUL3]
GtoPdb - - 5.2 pEC50 - - - Mol Pharmacol (2012) 81: 631-42 [PMID:22282525]
FFA1 receptor in Human [GtoPdb: 225] [UniProtKB: O14842]
GtoPdb - - 5.1 pEC50 - - - J Biol Chem (2003) 278: 11303-11 [PMID:12496284];
Biochem Biophys Res Commun (2003) 301: 406-10 [PMID:12565875];
Nature (2003) 422: 173-6 [PMID:12629551]

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]