ONO-AE1-437 [Ligand Id: 8541] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL292964 |
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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 | Affinity for human Prostanoid IP receptor expressed in CHO cells | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2033-2035 [PMID:11454474] |
| EP1 receptor/Prostaglandin E2 receptor EP1 subtype in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2181] [GtoPdb: 340] [UniProtKB: P35375] | ||||||||
| ChEMBL | Affinity for mouse Prostanoid EP1 receptor expressed in CHO cells | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2033-2035 [PMID:11454474] |
| ChEMBL | Displacement of [3H]-PGE2 from mouse EP1 receptor expressed in CHO cells after 20 mins by liquid scintillation counter | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2012) 20: 702-713 [PMID:22204740] |
| EP2 receptor/Prostaglandin E2 receptor EP2 subtype in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116] | ||||||||
| ChEMBL | Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA | F | 5 | pEC50 | 10000 | nM | EC50 | J Med Chem (2019) 62: 4731-4741 [PMID:30964292] |
| ChEMBL | Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay | F | 6.21 | pEC50 | 610 | nM | EC50 | J Med Chem (2019) 62: 4731-4741 [PMID:30964292] |
| EP2 receptor/Prostaglandin E2 receptor EP2 subtype in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2488] [GtoPdb: 341] [UniProtKB: Q62053] | ||||||||
| ChEMBL | Affinity for mouse Prostanoid EP2 receptor expressed in CHO cells | B | 6.21 | pKi | 620 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2033-2035 [PMID:11454474] |
| ChEMBL | Binding affinity to mouse EP2 receptor by competitive binding assay | B | 6.21 | pKi | 620 | nM | Ki | J Med Chem (2010) 53: 4332-4353 [PMID:20218623] |
| ChEMBL | Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter | B | 6.21 | pKi | 620 | nM | Ki | Bioorg Med Chem (2012) 20: 702-713 [PMID:22204740] |
| EP3 receptor/Prostaglandin E2 receptor EP3 subtype in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4336] [GtoPdb: 342] [UniProtKB: P30557] | ||||||||
| ChEMBL | Affinity for mouse Prostanoid EP3 receptor expressed in CHO cells | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2033-2035 [PMID:11454474] |
| ChEMBL | Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counter | B | 7.25 | pKi | 56 | nM | Ki | Bioorg Med Chem (2012) 20: 702-713 [PMID:22204740] |
| EP4 receptor/Prostaglandin E2 receptor EP4 subtype in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408] | ||||||||
| ChEMBL | Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method | B | 9.4 | pKi | 0.4 | nM | Ki | J Med Chem (2019) 62: 4731-4741 [PMID:30964292] |
| ChEMBL | Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA | F | 9.85 | pEC50 | 0.14 | nM | EC50 | J Med Chem (2019) 62: 4731-4741 [PMID:30964292] |
| ChEMBL | Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay | F | 11 | pEC50 | 0.01 | nM | EC50 | J Med Chem (2019) 62: 4731-4741 [PMID:30964292] |
| EP4 receptor/Prostaglandin E2 receptor EP4 subtype in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2489] [GtoPdb: 343] [UniProtKB: P32240] | ||||||||
| GtoPdb | - | - | 9.15 | pKi | 0.71 | nM | Ki | Osteoarthr Cartil (2003) 11: 644-52 [PMID:12954235] |
| ChEMBL | Affinity for mouse Prostanoid EP4 receptor expressed in CHO cells | B | 9.15 | pKi | 0.7 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2033-2035 [PMID:11454474] |
| ChEMBL | Binding affinity to mouse EP4 receptor by competitive binding assay | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (2010) 53: 4332-4353 [PMID:20218623] |
| ChEMBL | Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation counter | B | 9.15 | pKi | 0.7 | nM | Ki | Bioorg Med Chem (2012) 20: 702-713 [PMID:22204740] |
| ChEMBL | Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor | F | 8.8 | pEC50 | 1.6 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 2033-2035 [PMID:11454474] |
| EP4 receptor/Prostaglandin E2 receptor EP4 subtype in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4086] [GtoPdb: 343] [UniProtKB: P43114] | ||||||||
| ChEMBL | Agonist activity at rat EP4 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay | F | 8.85 | pEC50 | 1.4 | nM | EC50 | Bioorg Med Chem (2012) 20: 702-713 [PMID:22204740] |
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]
