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 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]
