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ChEMBL ligand: CHEMBL464982 (18:3(N-6), (6z,9z,12z-octadecatrienoic acid, C18:3 (n-6), Delta-linolenic acid, Efamast 40, Efamast 80, Epoc, Epogam, Epogam 40, Epogam 80, Epogam paed, Gamma-linolenate, .gamma.-linolenic acid, Gamma linolenic acid, Gammalinolenic acid, Gammolin, Gam-o, Gamolenic acid, Gamolenic-acid, Gamophase, Kentogam, Lin-gam, NDI 609, Sonova 400, Unigam) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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] |
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 | F | 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 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]