ONO-8130 [Ligand Id: 11536] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3939289 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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| EP1 receptor/Prostanoid EP1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2181] [GtoPdb: 340] [UniProtKB: P35375] | ||||||||
| GtoPdb | Measuring antagonism of agonist-induced intracellular calcium elevation in cells expressing mouse EP1 receptor. | - | 8.03 | pIC50 | 9.3 | nM | IC50 | US9181187B2. Therapeutic agent for urinary excretion disorder (2015) |
| ChEMBL | Inhibition Assay: The cells expressing mouse EP1 receptor were seeded at 104 cells/well in 96-well plates and cultured for 2 days with 10% Fetal Bovine Serum (FBS)/alpha Modified Eagle Medium (alphaMEM) in the incubator (37° C., 5% CO2). The cells were washed with phosphate buffer, and load buffer (10% FBS/αMEM containing Fura2/AM (5 uM), indomethacin (20 uM) and probenecid (2.5 mM)) was then added to each well and cells were left standing for 1 hour. Load buffer of each well was discarded and assay buffer (Hank's Balanced Salt Solution (HBSS) containing indomethacin (2.5 mM), probenecid (2.5 mM), HEPES-NaOH (10 mM) and 0.1% (w/v) Bovine Serum Albumin (BSA)) was added to each well and plates were left at room temperature in a dark room for 1 hour. Afterwards, compounds of the present invention (10 uL) or PGE2 (10 uL) prepared with assay buffer was added to each well and intracellular calcium concentrations were measured using a Fluorescence Drug Screening System. | B | 8.03 | pIC50 | 9.3 | nM | IC50 | US-9181187-B2. Therapeutic agent for urinary excretion disorder (2015) |
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]
