CJ-042794 [Ligand Id: 5857] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL591666 (CJ-142794) |
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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 | Antagonist activity at human EP1 receptor | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1186-1192 [PMID:28169162] |
| EP2 receptor/Prostanoid EP2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116] | ||||||||
| ChEMBL | Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6336-6340 [PMID:21930381] |
| ChEMBL | Antagonist activity at human EP2 receptor | B | 6.15 | pIC50 | 709 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1186-1192 [PMID:28169162] |
| EP3 receptor/Prostanoid EP3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115] | ||||||||
| ChEMBL | Antagonist activity at human EP3 receptor | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1186-1192 [PMID:28169162] |
| EP4 receptor/Prostanoid EP4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408] | ||||||||
| ChEMBL | Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay | F | 8.75 | pKd | 1.78 | nM | Kd | Bioorg Med Chem Lett (2017) 27: 1186-1192 [PMID:28169162] |
| GtoPdb | - | - | 8.51 | pKi | 3.1 | nM | Ki | Eur J Pharmacol (2008) 580: 116-21 [PMID:18031725] |
| ChEMBL | Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay | F | 7.42 | pIC50 | 38.2 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1186-1192 [PMID:28169162] |
| ChEMBL | Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP accumulation by bead-based proximity assay | F | 7.89 | pIC50 | 13 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6336-6340 [PMID:21930381] |
| ChEMBL | Displacement of [3H]-PGE2 from human EP4 receptor expressed in HEK293 cells | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6336-6340 [PMID:21930381] |
| ChEMBL | Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes | B | 8.18 | pIC50 | 6.59 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1186-1192 [PMID:28169162] |
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]
