lauric acid [Ligand Id: 5534] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL108766 (Dodecanoic Acid, Dodecanoic Acid Anion, Lauric Acid) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| FFA1 receptor/Free fatty acid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4422] [GtoPdb: 225] [UniProtKB: O14842] | ||||||||
| ChEMBL | Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in Flp-In T-Rex 293 cells assessed as induction of Ca2+ mobilization after 45 mins by Fura2-AM dye-based fluorescence assay | F | 4.94 | pEC50 | 11481.54 | nM | EC50 | Medchemcomm (2017) 8: 1360-1365 [PMID:30108848] |
| ChEMBL | Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay | B | 5.1 | pEC50 | 7943.28 | nM | EC50 | J Med Chem (2016) 59: 4849-4858 [PMID:27074625] |
| ChEMBL | Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay | F | 6.12 | pEC50 | 758.58 | nM | EC50 | J Med Chem (2016) 59: 4849-4858 [PMID:27074625] |
| FFA4 receptor/G-protein coupled receptor 120 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3] | ||||||||
| ChEMBL | Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA4 receptor expressed in HEK293T cells assessed as induction of beta-arrestin-2 recruitment after 5 mins by BRET assay | F | 5.12 | pEC50 | 7585.78 | nM | EC50 | Medchemcomm (2017) 8: 1360-1365 [PMID:30108848] |
| 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 | 5.66 | pKi | 2170 | 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 | 4.98 | pEC50 | 10500 | nM | EC50 | J Med Chem (2020) 63: 15399-15409 [PMID:33267584] |
| ChEMBL | Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method | F | 4.98 | pEC50 | 10471.29 | nM | EC50 | Medchemcomm (2017) 8: 1360-1365 [PMID:30108848] |
| GtoPdb | - | - | 5.05 | pEC50 | 9000 | nM | EC50 | J Biol Chem (2006) 281: 34457-64 [PMID:16966319] |
| 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 | 5.05 | pEC50 | 8870 | nM | EC50 | J Med Chem (2020) 63: 2391-2410 [PMID:31721581] |
| ChEMBL | Agonist activity at human GPR84 expressed in CHO cells assessed as reduction in forskolin-stimulated cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 20 mins by cAMP assay | F | 5.06 | pEC50 | 8800 | nM | EC50 | J Med Chem (2020) 63: 15399-15409 [PMID:33267584] |
| ChEMBL | Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 20 mins followed by forskolin-induction and measured after 20 mins | F | 5.06 | pEC50 | 8709.64 | nM | EC50 | Medchemcomm (2017) 8: 1360-1365 [PMID:30108848] |
| 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 | 5.46 | pEC50 | 3490 | 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 | 4.52 | pIC50 | 30000 | 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 | 4.52 | pIC50 | 30000 | 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 | 4.52 | pIC50 | 30000 | nM | IC50 | Med Chem Res (2013) 22: 3126-3133 |
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]
