γ-linolenic acid [Ligand Id: 4710] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL464982 (Unigam, Epoc, Epogam 80, Lin-Gam, Epogam Paed, Gamophase, .gamma.-linolenic acid, Epogam 40, Gammolin, Gamolenic Acid, Kentogam, 18:3(N-6), Efamast 40, Efamast 80, NDI 609, Epogam, Gam-O)
  • coagulation factor VII/Coagulation factor VII/tissue factor in Human [ChEMBL: CHEMBL2095194] [GtoPdb: 2363] [UniProtKB: P08709P13726]
  • This target only has 0 pki data point
1 CHEMBL464982_lig_chart_1 Coagulation factor VII/tissue factor Human
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  • FFA1 receptor/Free fatty acid receptor 1 in Human [ChEMBL: CHEMBL4422] [GtoPdb: 225] [UniProtKB: O14842]
  • This target only has 0 pki data point
2 CHEMBL464982_lig_chart_2 Free fatty acid receptor 1 Human
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  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
  • This target only has 0 pki data point
3 CHEMBL464982_lig_chart_3 Peroxisome proliferator-activated receptor alpha Human
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  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
  • This target only has 0 pki data point
4 CHEMBL464982_lig_chart_4 Peroxisome proliferator-activated receptor delta Human
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
  • This target only has 0 pki data point
5 CHEMBL464982_lig_chart_5 Peroxisome proliferator-activated receptor gamma Human
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  • steroid 5 alpha-reductase 2/Steroid 5-alpha-reductase 2 in Human [ChEMBL: CHEMBL1856] [GtoPdb: 2633] [UniProtKB: P31213]
  • This target only has 0 pki data point
6 CHEMBL464982_lig_chart_6 Steroid 5-alpha-reductase 2 Human
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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 VII/tissue factor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095194] [GtoPdb: 2363] [UniProtKB: P08709P13726]
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]
FFA1 receptor/Free fatty acid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4422] [GtoPdb: 225] [UniProtKB: O14842]
ChEMBL Agonist activity at human FFAR1 expressed in CHO-K1 cells assessed as calcium flux measured for 100 secs by FLIPR assay B 5.34 pEC50 4620 nM EC50 Eur. J. Med. Chem. (2016) 109: 157-172 [PMID:26774923]
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
ChEMBL Inhibition of PPAR-alpha (unknown origin) by SPA assay B 6.57 pIC50 270 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 6.57 pIC50 270 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 6.12 pIC50 750 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 5.66 pIC50 2200 nM IC50 Med Chem Res (2013) 22: 3126-3133
steroid 5 alpha-reductase 2/Steroid 5-alpha-reductase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1856] [GtoPdb: 2633] [UniProtKB: P31213]
ChEMBL In Vitro Inhibition Assay: This work was performed at the MDS Pharma Services, Pharmacology Laboratories, Taiwan. The assay was an in vitro evaluation of the ability of an extract or a pure compound to inhibit the steroid 5alpha -reductase enzyme from metabolizing testosterone into dihydrotestosterone. This is an enzyme-immunoassay (EIA) for quantitative determination of testosterone in human serum or plasma. The significance of this type of inhibition is that it can lead to eradication of benign prostatic hyperplasia (BPH). Two distinct isozymes are found in mice, rats, monkeys and humans: type 1 and II. Each of these isozymes is differentially expressed in tissues and developmental stages. In human, type 1 steroid 5alpha -reductase is predominant in the sebaceous glands of most regions of skin, including scalp and liver and is responsible for approximately one third of circulating DHT. Inhibitors of steroid 5alpha -reductase may be of benefit in the treatment of androgenetic alopecia. B 4.85 pIC50 14000 nM IC50 US-9061023-B2. Management and treatment of benign prostatic hyperplasia (2015)

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]