selexipag [Ligand Id: 7552] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL238804 (ACT-293987, NS-304, Selexipag, Uptravi) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| DP1 receptor/Prostanoid DP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4427] [GtoPdb: 338] [UniProtKB: Q13258] | ||||||||
| ChEMBL | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method | F | 7 | pEC50 | 100 | nM | EC50 | J Med Chem (2017) 60: 913-927 [PMID:28072531] |
| IP receptor/Prostanoid IP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119] | ||||||||
| GtoPdb | - | - | 6.59 | pKi | 260 | nM | Ki | J Pharmacol Exp Ther (2007) 322: 1181-8 [PMID:17545310] |
| ChEMBL | Agonist activity at IP receptor in human primary platelets assessed as inhibition of ADP-induced platelet aggregation | B | 7.21 | pIC50 | 62 | nM | IC50 | J Med Chem (2017) 60: 913-927 [PMID:28072531] |
| ChEMBL | Agonist activity at recombinant human IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method | F | 8.22 | pEC50 | 6 | nM | EC50 | J Med Chem (2017) 60: 913-927 [PMID:28072531] |
| IP receptor/Prostanoid IP receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3322] [GtoPdb: 345] [UniProtKB: P43253] | ||||||||
| GtoPdb | - | - | 5.68 | pKi | 2100 | nM | Ki | J Pharmacol Exp Ther (2007) 322: 1181-8 [PMID:17545310] |
| ChEMBL | Agonist activity at recombinant rat IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method | F | 6.7 | pEC50 | 200 | nM | EC50 | J Med Chem (2017) 60: 913-927 [PMID:28072531] |
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]
