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 34:
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]
