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 human PGI2 receptor assessed as inhibition of ADP-induced platelet aggregation | B | 5.19 | pIC50 | 6400 | nM | IC50 | J Med Chem (2020) 63: 15153-15186 [PMID:33314936] |
| 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] |
| AT1 receptor/Type-1 angiotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: AGTR1 | F | 5 | pIC50 | >10000 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
