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ChEMBL ligand: CHEMBL107498 (Decanoic Acid, Decanoic Acid Anion) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | F | 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 | F | 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 | F | 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 | F | 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 | F | 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 | F | 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 | F | 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 | F | 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 | F | 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 | Binding affinity to GST-tagged PPARG LBD (unknown origin) by Fluormone Pan-PPAR Green tracer based TR-FRET assay | B | 4.66 | pKi | 22000 | nM | Ki | J Med Chem (2021) 64: 1018-1036 [PMID:33423463] |
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 | Partial agonist activity at full length human PPARG expressed in African green monkey COS7 cells assessed as increase in receptor activation incubated for 24 hrs by luciferase reporter assay | B | 5.12 | pEC50 | 7600 | nM | EC50 | J Med Chem (2021) 64: 1018-1036 [PMID:33423463] |
ChEMBL data shown on this page come from version 32:
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]