decanoic acid [Ligand Id: 5532] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL107498 (Decanoic Acid, Decanoic Acid Anion)
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  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
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  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 5.75 pKi 1780 nM Ki J Med Chem (2020) 63: 2391-2410 [PMID:31721581]
ChEMBL Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting method B 4.32 pEC50 48000 nM EC50 J Med Chem (2020) 63: 2391-2410 [PMID:31721581]
ChEMBL Agonist activity at recombinant human GPR84 expressed in CHO cells co-expressing Galpha16/Gqs5/Gqo5/Gqi9 assessed as increase in calcium mobilization measured for 20 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay B 4.32 pEC50 48000 nM EC50 J Med Chem (2020) 63: 2391-2410 [PMID:31721581]
ChEMBL Agonist activity at recombinant human N-terminally HA-tagged GPR84 expressed in CHO cells co-expressing Gqi5 assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assay B 4.52 pEC50 30000 nM EC50 J Med Chem (2020) 63: 2391-2410 [PMID:31721581]
ChEMBL Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric method B 4.6 pEC50 25000 nM EC50 J Med Chem (2020) 63: 2391-2410 [PMID:31721581]
ChEMBL Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assay B 4.7 pEC50 20000 nM EC50 J Med Chem (2020) 63: 2391-2410 [PMID:31721581]
ChEMBL Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assay B 5 pEC50 10000 nM EC50 J Med Chem (2020) 63: 2391-2410 [PMID:31721581]
ChEMBL Agonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assay B 5 pEC50 10000 nM EC50 J Med Chem (2017) 60: 3636-3655 [PMID:28406627]
ChEMBL Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay B 5.13 pEC50 7420 nM EC50 J Med Chem (2017) 60: 3636-3655 [PMID:28406627]
ChEMBL Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay B 5.22 pEC50 6080 nM EC50 J Med Chem (2017) 60: 3636-3655 [PMID:28406627]
ChEMBL Agonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method B 5.34 pEC50 4600 nM EC50 J Med Chem (2020) 63: 2391-2410 [PMID:31721581]
ChEMBL Agonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin addition and measured after 20 mins B 5.34 pEC50 4600 nM EC50 J Med Chem (2020) 63: 2391-2410 [PMID:31721581]
ChEMBL Agonist activity at human N-terminal-FLAG-tagged human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated fro 20 mins followed by forskolin addition measured after 20 mins B 5.35 pEC50 4500 nM EC50 J Med Chem (2017) 60: 3636-3655 [PMID:28406627]
GtoPdb - - 5.4 pEC50 - - - J Biol Chem (2006) 281: 34457-64 [PMID:16966319];
J Biomol Screen (2013) 18: 599-609 [PMID:23396314]
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 28:

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]