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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| 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 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]
