evatanepag [Ligand Id: 1929] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL563646 (CP-533,536, CP-533536, Evatanepag) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| IP receptor/Prostacyclin 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] |
| EP1 receptor/Prostaglandin E2 receptor EP1 subtype 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/Prostaglandin E2 receptor EP2 subtype 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/Prostaglandin E2 receptor EP2 subtype 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/Prostaglandin E2 receptor EP3 subtype 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/Prostaglandin E2 receptor EP4 subtype 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/Prostaglandin E2 receptor EP4 subtype 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] |
ChEMBL data shown on this page come from version 36:
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]
