treprostinil [Ligand Id: 5820] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1237119 (15-AU-81, 15AU81, L-606, LRX -15, LRX-15, Remodulin, Rumodolin, Treprostinil, Treprostinilo, Tresprostinil, Tyvaso, Tyvaso dpi, Uniprost, UT-15) |
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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] | ||||||||
| GtoPdb | - | - | 8.4 | pKi | - | - | - |
Biochem Pharmacol (2012) 84: 68-75 [PMID:22480736]; Prostaglandins Leukot Essent Fatty Acids (2015) 95: 19-29 [PMID:25542069] |
| ChEMBL | Agonist activity at human DP1 expressed in human 1321N1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis | F | 9.22 | pEC50 | 0.6 | nM | EC50 | Eur J Med Chem (2022) 231: 114154-114154 [PMID:35124532] |
| EP1 receptor/Prostanoid EP1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995] | ||||||||
| GtoPdb | - | - | 6.7 | pKi | - | - | - | Biochem Pharmacol (2012) 84: 68-75 [PMID:22480736] |
| ChEMBL | Agonist activity at human EP1 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis | F | 6.55 | pEC50 | 285 | nM | EC50 | Eur J Med Chem (2022) 231: 114154-114154 [PMID:35124532] |
| EP2 receptor/Prostanoid EP2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116] | ||||||||
| GtoPdb | - | - | 8.4 | pKi | - | - | - |
Biochem Pharmacol (2012) 84: 68-75 [PMID:22480736]; Prostaglandins Leukot Essent Fatty Acids (2015) 95: 19-29 [PMID:25542069] |
| ChEMBL | Agonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis | F | 8.21 | pEC50 | 6.2 | nM | EC50 | Eur J Med Chem (2022) 231: 114154-114154 [PMID:35124532] |
| IP receptor/Prostanoid IP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119] | ||||||||
| GtoPdb | - | - | 7.49 | pKi | - | - | - | Biochem Pharmacol (2012) 84: 68-75 [PMID:22480736] |
| GtoPdb | - | - | 8.72 | pEC50 | - | - | - |
Biochem Pharmacol (2012) 84: 68-75 [PMID:22480736]; N Engl J Med (2021) 384: 325-334 [PMID:33440084] |
| ChEMBL | Agonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis | F | 8.72 | pEC50 | 1.9 | nM | EC50 | Eur J Med Chem (2022) 231: 114154-114154 [PMID:35124532] |
| EP3 receptor in Human [GtoPdb: 342] [UniProtKB: P43115] | ||||||||
| GtoPdb | - | - | 5.6 | pKi | 2500 | nM | Ki | Biochem Pharmacol (2012) 84: 68-75 [PMID:22480736] |
| EP4 receptor in Human [GtoPdb: 343] [UniProtKB: P35408] | ||||||||
| GtoPdb | - | - | 6.1 | pKi | 800 | nM | Ki | Biochem Pharmacol (2012) 84: 68-75 [PMID:22480736] |
| GtoPdb | - | - | 6.7 | pEC50 | 200 | nM | EC50 | Biochem Pharmacol (2012) 84: 68-75 [PMID:22480736] |
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]
