MRE-269 [Ligand Id: 5852] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL239226 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| DP1 receptor/Prostanoid DP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4427] [GtoPdb: 338] [UniProtKB: Q13258] | ||||||||
| ChEMBL | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method | F | 6.81 | pEC50 | 154 | nM | EC50 | J Med Chem (2017) 60: 913-927 [PMID:28072531] |
| IP receptor/Prostanoid IP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119] | ||||||||
| GtoPdb | - | - | 7.7 | pKi | 20 | nM | Ki |
J Pharmacol Exp Ther (2007) 322: 1181-8 [PMID:17545310]; Prostaglandins Other Lipid Mediat (2013) 107: 48-55 [PMID:23850788] |
| ChEMBL | Agonist activity at IP receptor in human primary platelets assessed as inhibition of ADP-induced platelet aggregation | B | 6.54 | pIC50 | 288 | nM | IC50 | J Med Chem (2017) 60: 913-927 [PMID:28072531] |
| ChEMBL | Agonist activity at recombinant human IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method | F | 7.66 | pEC50 | 22 | nM | EC50 | J Med Chem (2017) 60: 913-927 [PMID:28072531] |
| IP receptor in Rat [GtoPdb: 345] [UniProtKB: P43253] | ||||||||
| GtoPdb | - | - | 6.66 | pKi | 220 | nM | Ki | J Pharmacol Exp Ther (2007) 322: 1181-8 [PMID:17545310] |
| EP2 receptor in Human [GtoPdb: 341] [UniProtKB: P43116] | ||||||||
| GtoPdb | - | - | 5.24 | pKi | 5800 | nM | Ki | J Pharmacol Exp Ther (2007) 322: 1181-8 [PMID:17545310] |
| EP4 receptor in Human [GtoPdb: 343] [UniProtKB: P35408] | ||||||||
| GtoPdb | - | - | 5.31 | pKi | 4900 | nM | Ki | J Pharmacol Exp Ther (2007) 322: 1181-8 [PMID:17545310] |
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]
