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)
  • DP1 receptor/Prostanoid DP receptor in Human [ChEMBL: CHEMBL4427] [GtoPdb: 338] [UniProtKB: Q13258]
Created with Highcharts 10.3.3ValuesChart context menuProstanoid DP receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • EP1 receptor/Prostanoid EP1 receptor in Human [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995]
Created with Highcharts 10.3.3ValuesChart context menuProstanoid EP1 receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
  • EP2 receptor/Prostanoid EP2 receptor in Human [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116]
Created with Highcharts 10.3.3ValuesChart context menuProstanoid EP2 receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • IP receptor/Prostanoid IP receptor in Human [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119]
Created with Highcharts 10.3.3ValuesChart context menuProstanoid IP receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • EP3 receptor in Human [GtoPdb: 342] [UniProtKB: P43115]
Created with Highcharts 10.3.3ValuesChart context menuEP3 receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • EP4 receptor in Human [GtoPdb: 343] [UniProtKB: P35408]
Created with Highcharts 10.3.3ValuesChart context menuEP4 receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
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 35:

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]