α-linolenic acid [Ligand Id: 1049] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL8739 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| coagulation factor VII/coagulation factor III, tissue factor/Coagulation factor VII/tissue factor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095194] [GtoPdb: 2363, 3192] [UniProtKB: P08709, P13726] | ||||||||
| ChEMBL | Inhibition of amidolytic activity of human tissue factor/human factor 7a | B | 4.52 | pIC50 | 30000 | nM | IC50 | J Nat Prod (1998) 61: 1352-1355 [PMID:9834151] |
| COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219] | ||||||||
| ChEMBL | Inhibition of COX-1 (unknown origin) using arachidonic acid as substrate assessed as formation of prostanoid products preincubated for 10 mins prior to substrate addition measured after 2 mins by Ellman's method | B | 5.4 | pKi | 4000 | nM | Ki | J Med Chem (2013) 56: 8377-8388 [PMID:24088053] |
| Cyclooxygenase-1 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2860] [UniProtKB: O62664] | ||||||||
| ChEMBL | Inhibition of bovine COX1-mediated prostaglandin biosynthesis using [1-14C]arachidonic acid | B | 4.03 | pIC50 | 93000 | nM | IC50 | J Nat Prod (2001) 64: 745-749 [PMID:11421736] |
| Cyclooxygenase-2 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4102] [UniProtKB: P79208] | ||||||||
| ChEMBL | Inhibition of sheep COX2-mediated prostaglandin biosynthesis using [1-14C]arachidonic acid | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Nat Prod (2001) 64: 745-749 [PMID:11421736] |
| CYP19A1/Cytochrome P450 19A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1978] [GtoPdb: 1362] [UniProtKB: P11511] | ||||||||
| ChEMBL | Inhibition of aromatase in human placental microsomes by radiometric method | B | 4.35 | pIC50 | 44200 | nM | IC50 | J Nat Prod (2006) 69: 700-703 [PMID:16643058] |
| FFA1 receptor/Free fatty acid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4422] [GtoPdb: 225] [UniProtKB: O14842] | ||||||||
| ChEMBL | Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay | F | 4.96 | pEC50 | 11090 | nM | EC50 | Eur J Med Chem (2018) 158: 123-133 [PMID:30212763] |
| ChEMBL | Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay | F | 5.28 | pEC50 | 5200 | nM | EC50 | J Med Chem (2008) 51: 7640-7644 [PMID:19007110] |
| ChEMBL | Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay | F | 5.5 | pEC50 | 3162.28 | nM | EC50 | J Med Chem (2016) 59: 2841-2846 [PMID:26928019] |
| ChEMBL | Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay | F | 5.52 | pEC50 | 3000 | nM | EC50 | J Med Chem (2016) 59: 2841-2846 [PMID:26928019] |
| ChEMBL | Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay | F | 5.54 | pEC50 | 2884.03 | nM | EC50 | J Med Chem (2012) 55: 4511-4515 [PMID:22519963] |
| GtoPdb | - | - | 5.7 | 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] |
| FFA4 receptor/G-protein coupled receptor 120 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3] | ||||||||
| ChEMBL | Agonist activity at GPR120 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 5 mins by BRET assay | F | 5.49 | pEC50 | 3235.94 | nM | EC50 | J Med Chem (2012) 55: 4511-4515 [PMID:22519963] |
| GtoPdb | - | - | 5.5 | pEC50 | - | - | - | J Med Chem (2012) 55: 4511-5 [PMID:22519963] |
| ChEMBL | Agonist activity at human GPR120-G-alpha-16 fusion protein expressed in Flp-in HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay | F | 5.59 | pEC50 | 2600 | nM | EC50 | J Med Chem (2008) 51: 7640-7644 [PMID:19007110] |
| FFA4 receptor in Rat [GtoPdb: 127] [UniProtKB: Q2AC31] | ||||||||
| GtoPdb | - | - | 5.06 | pEC50 | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2008) 377: 515-22 [PMID:18320172] |
| Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869] | ||||||||
| ChEMBL | Binding affinity to PPAR-alpha (unknown origin) by fluorescence-based assay | B | 8.1 | pKd | 7.9 | nM | Kd | Med Chem Res (2009) 18: 8-19 |
| ChEMBL | Inhibition of PPAR-alpha (unknown origin) by SPA assay | B | 5.92 | pIC50 | 1200 | nM | IC50 | Med Chem Res (2009) 18: 8-19 |
| ChEMBL | Displacement of [3H]GW2331 from Homo sapiens (human) PPARalpha receptor by scintillation proximity assay | B | 5.92 | pIC50 | 1200 | 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 | 4.8 | pIC50 | 16000 | 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 | Binding affinity to PPARgamma | B | 5.7 | pKd | 2000 | nM | Kd | J Med Chem (2012) 55: 4027-4061 [PMID:22260081] |
| ChEMBL | Displacement of [3H]BRL49653 from Homo sapiens (human) PPARgamma receptor by scintillation proximity assay | B | 5.22 | pIC50 | 6000 | nM | IC50 | Med Chem Res (2013) 22: 3126-3133 |
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]
