ONO-AE1-437 [Ligand Id: 8541] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL292964
  • EP1 receptor/Prostanoid EP1 receptor in Mouse [ChEMBL: CHEMBL2181] [GtoPdb: 340] [UniProtKB: P35375]
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  • EP2 receptor/Prostanoid EP2 receptor in Human [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116]
  • EP2 receptor/Prostanoid EP2 receptor in Mouse [ChEMBL: CHEMBL2488] [GtoPdb: 341] [UniProtKB: Q62053]
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  • EP3 receptor/Prostanoid EP3 receptor in Mouse [ChEMBL: CHEMBL4336] [GtoPdb: 342] [UniProtKB: P30557]
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  • EP4 receptor/Prostanoid EP4 receptor in Human [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408]
  • EP4 receptor/Prostanoid EP4 receptor in Mouse [ChEMBL: CHEMBL2489] [GtoPdb: 343] [UniProtKB: P32240]
  • EP4 receptor/Prostanoid EP4 receptor in Rat [ChEMBL: CHEMBL4086] [GtoPdb: 343] [UniProtKB: P43114]
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  • IP receptor/Prostanoid IP receptor in Human [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119]
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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 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 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]