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 |
|---|---|---|---|---|---|---|---|---|
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
