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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 |
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EP1 receptor/Prostanoid EP1 receptor 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/Prostanoid EP2 receptor 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/Prostanoid EP2 receptor 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/Prostanoid EP3 receptor 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/Prostanoid EP4 receptor 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/Prostanoid EP4 receptor 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/Prostanoid EP4 receptor 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] |
IP receptor/Prostanoid IP 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] |
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]