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 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]