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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 |
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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 |
ChEMBL | Agonist activity at human PPARalpha expressed in HEK293 cells by luciferase/beta-galactosidase reporter gene assay | B | 4.89 | pEC50 | 13000 | nM | EC50 | J Med Chem (2022) 65: 1961-1978 [PMID:35089724] |
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 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]