evatanepag [Ligand Id: 1929] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL563646 (Evatanepag, CP-533536)
  • EP1 receptor/Prostanoid EP1 receptor in Human [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995]
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  • EP2 receptor/Prostanoid EP2 receptor in Human [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116]
  • EP2 receptor/Prostanoid EP2 receptor in Rat [ChEMBL: CHEMBL4909] [GtoPdb: 341] [UniProtKB: Q62928]
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  • EP3 receptor/Prostanoid EP3 receptor in Human [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115]
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  • EP4 receptor/Prostanoid EP4 receptor in Human [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408]
  • EP4 receptor/Prostanoid EP4 receptor in Rat [ChEMBL: CHEMBL4086] [GtoPdb: 343] [UniProtKB: P43114]
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  • IP receptor/Prostanoid IP receptor in Human [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
EP1 receptor/Prostanoid EP1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995]
ChEMBL Binding affinity to EP1 receptor (unknown origin) B 5.55 pKi >2800 nM Ki J. Med. Chem. (2014) 57: 4454-4465 [PMID:24279689]
EP2 receptor/Prostanoid EP2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116]
ChEMBL Binding affinity to EP2 receptor (unknown origin) by competitive binding assay B 7.3 pKi 50 nM Ki J. Med. Chem. (2014) 57: 4454-4465 [PMID:24279689]
ChEMBL Agonist activity at EP2 receptor (unknown origin) by functional assay B 8.3 pEC50 5 nM EC50 J. Med. Chem. (2014) 57: 4454-4465 [PMID:24279689]
EP2 receptor/Prostanoid EP2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4909] [GtoPdb: 341] [UniProtKB: Q62928]
GtoPdb - - 7.3 pIC50 50.1 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 2075-8 [PMID:19250823]
ChEMBL Inhibition of rat EP2 receptor expressed in HEK293 cells B 7.3 pIC50 50 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 2075-2078 [PMID:19250823]
GtoPdb - - 9.5 pEC50 0.3 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 2075-8 [PMID:19250823]
ChEMBL Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release F 9.52 pEC50 0.3 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 2075-2078 [PMID:19250823]
EP3 receptor/Prostanoid EP3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115]
ChEMBL Binding affinity to EP3 receptor (unknown origin) B 5.55 pKi >2800 nM Ki J. Med. Chem. (2014) 57: 4454-4465 [PMID:24279689]
EP4 receptor/Prostanoid EP4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408]
ChEMBL Binding affinity to EP4 receptor (unknown origin) B 5.49 pKi >3200 nM Ki J. Med. Chem. (2014) 57: 4454-4465 [PMID:24279689]
GtoPdb - - 8.6 pKi 2.51 nM Ki Life Sci. (2008) 82: 226-32 [PMID:18155068]
EP4 receptor/Prostanoid EP4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4086] [GtoPdb: 343] [UniProtKB: P43114]
ChEMBL Inhibition of rat EP4 receptor expressed in HEK293 cells B 5.49 pIC50 >3200 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 2075-2078 [PMID:19250823]
IP receptor/Prostanoid IP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119]
ChEMBL Binding affinity to prostanoid IP receptor (unknown origin) B 5.49 pKi >3200 nM Ki J. Med. Chem. (2014) 57: 4454-4465 [PMID:24279689]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]