PGE2 [Ligand Id: 1883] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL548 (Dinoprostone beta-cyclodextrin clathrate, Prostaglandin e2, Prepidil, U-12062, U-12,062, NSC-196514, Cervidil, Propess, Prostin e2, NSC-165560, Dinoprostone)
  • EP1 receptor/Prostanoid EP1 receptor in Human [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995]
  • EP1 receptor/Prostanoid EP1 receptor in Mouse [ChEMBL: CHEMBL2181] [GtoPdb: 340] [UniProtKB: P35375]
  • EP1 receptor in Rat [GtoPdb: 340] [UniProtKB: P70597]
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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]
  • EP2 receptor/Prostanoid EP2 receptor in Rat [ChEMBL: CHEMBL4909] [GtoPdb: 341] [UniProtKB: Q62928]
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  • EP3 receptor/Prostanoid EP3 receptor in Human [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115]
  • EP3 receptor/Prostanoid EP3 receptor in Mouse [ChEMBL: CHEMBL4336] [GtoPdb: 342] [UniProtKB: P30557]
  • EP3 receptor in Rat [GtoPdb: 342] [UniProtKB: P34980]
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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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  • FP receptor/Prostanoid FP receptor in Human [ChEMBL: CHEMBL1987] [GtoPdb: 344] [UniProtKB: P43088]
  • FP receptor in Mouse [GtoPdb: 344] [UniProtKB: P43117]
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  • IP receptor/Prostanoid IP receptor in Human [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119]
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  • OAT6/Solute carrier family 22 member 20 in Mouse [ChEMBL: CHEMBL5269] [GtoPdb: 1037] [UniProtKB: Q80UJ1]
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  • Organic anion transporter 1/Solute carrier family 22 member 6 in Mouse [ChEMBL: CHEMBL5653] [GtoPdb: 1025] [UniProtKB: Q8VC69]
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  • DP1 receptor in Human [GtoPdb: 338] [UniProtKB: Q13258]
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  • DP2 receptor in Human [GtoPdb: 339] [UniProtKB: Q9Y5Y4]
  • DP2 receptor in Mouse [GtoPdb: 339] [UniProtKB: Q9Z2J6]
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  • TP receptor in Human [GtoPdb: 346] [UniProtKB: P21731]
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  • CatSper1 in Human [GtoPdb: 388] [UniProtKB: Q8NEC5]
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  • CatSper2 in Human [GtoPdb: 389] [UniProtKB: Q96P56]
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  • CatSper3 in Human [GtoPdb: 390] [UniProtKB: Q86XQ3]
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  • CatSper4 in Human [GtoPdb: 391] [UniProtKB: Q7RTX7]
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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 Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995]
ChEMBL Binding affinity to EP1 receptor (unknown origin) B 7.74 pKi 18 nM Ki J. Med. Chem. (2014) 57: 4454-4465 [PMID:24279689]
GtoPdb - - 8 pKi - - - Br J Pharmacol (2006) 148: 326-39 [PMID:16604093];
Biochim Biophys Acta (2000) 1483: 285-93 [PMID:10634944];
J Pharm Pharmacol (2002) 54: 539-47 [PMID:11999132]
ChEMBL Displacement of [3H]PGE2 from human EP1 receptor expressed in HEK293 cells B 8.04 pKi 9.1 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 4323-4327 [PMID:17531488]
ChEMBL Displacement of [3H]PGE2 from human EP1 receptor B 8.04 pKi 9.1 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 821-824 [PMID:18039575]
ChEMBL Binding affinity to EP1 receptor B 8.96 pIC50 1.1 nM IC50 J. Med. Chem. (2010) 53: 4332-4353 [PMID:20218623]
ChEMBL Agonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis B 8.43 pEC50 3.7 nM EC50 ACS Med. Chem. Lett. (2016) 7: 306-311 [PMID:26985320]
EP1 receptor/Prostanoid EP1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2181] [GtoPdb: 340] [UniProtKB: P35375]
GtoPdb - - 7.7 pKi - - - Br J Pharmacol (1997) 122: 217-24 [PMID:9313928];
Endocrinology (2000) 141: 1554-9 [PMID:10746663]
ChEMBL Displacement of [3H]-PGE2 from mouse EP1 receptor expressed in CHO cells after 20 mins by liquid scintillation counting B 8.22 pKi 6 nM Ki Bioorg. Med. Chem. Lett. (2012) 22: 396-401 [PMID:22119471]
ChEMBL Displacement of [3H]-PGE2 from mouse EP1 receptor expressed in CHO cells after 60 mins by scintillation counting B 8.22 pKi 6 nM Ki Bioorg. Med. Chem. (2012) 20: 2235-2251 [PMID:22386979]
EP1 receptor in Rat [GtoPdb: 340] [UniProtKB: P70597]
GtoPdb - - 7.7 pKi - - - Eur J Pharmacol (1997) 340: 227-41 [PMID:9537820]
EP2 receptor/Prostanoid EP2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116]
ChEMBL Binding affinity to EP2 receptor (unknown origin) by competitive binding assay B 7.42 pKi 38 nM Ki J. Med. Chem. (2014) 57: 4454-4465 [PMID:24279689]
GtoPdb - - 8.3 pKi 5.01 nM Ki Br J Pharmacol (2006) 148: 326-39 [PMID:16604093];
Biochim Biophys Acta (2000) 1483: 285-93 [PMID:10634944];
Mol Pharmacol (1999) 56: 545-51 [PMID:10462542]
ChEMBL Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells B 8.31 pKi 4.9 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 4323-4327 [PMID:17531488]
ChEMBL Binding affinity at human prostaglandin EP2 receptor B 8.31 pKi 4.9 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 6572-6575 [PMID:17931866]
ChEMBL Displacement of [3H]PGE2 from human EP2 receptor B 8.31 pKi 4.9 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 821-824 [PMID:18039575]
ChEMBL Binding affinity to human prostanoid EP2 receptor by radioligand displacement assay B 8.77 pKi 1.7 nM Ki Eur. J. Med. Chem. (2013) 63: 85-94 [PMID:23466604]
ChEMBL Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method B 8.99 pKi 1.03 nM Ki J Med Chem (2019) 62: 4731-4741 [PMID:30964292]
ChEMBL Binding affinity to EP2 receptor B 7.42 pIC50 37.7 nM IC50 J. Med. Chem. (2010) 53: 4332-4353 [PMID:20218623]
ChEMBL Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting B 8.4 pIC50 4 nM IC50 J Med Chem (2018) 61: 6869-6891 [PMID:29995405]
ChEMBL Binding affinity to human prostanoid EP2 receptor by radioligand displacement assay B 8.48 pIC50 3.3 nM IC50 Eur. J. Med. Chem. (2013) 63: 85-94 [PMID:23466604]
ChEMBL Displacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cells B 8.59 pIC50 2.6 nM IC50 Bioorg. Med. Chem. (2016) 24: 1793-1810 [PMID:26988801]
ChEMBL Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method B 8.59 pIC50 2.6 nM IC50 Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]
ChEMBL Binding affinity to human EP2 receptor (unknown origin) by radioligand displacement assay B 8.66 pIC50 2.2 nM IC50 Bioorg. Med. Chem. (2013) 21: 2764-2771 [PMID:23582449]
ChEMBL Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay B 6.46 pEC50 346 nM EC50 ACS Med. Chem. Lett. (2016) 7: 306-311 [PMID:26985320]
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 B 6.48 pEC50 331 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 B 8.03 pEC50 9.3 nM EC50 J Med Chem (2019) 62: 4731-4741 [PMID:30964292]
ChEMBL Agonist activity at EP2 receptor (unknown origin) by functional assay B 8.68 pEC50 2.1 nM EC50 J. Med. Chem. (2014) 57: 4454-4465 [PMID:24279689]
ChEMBL Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method B 8.72 pEC50 1.9 nM EC50 ACS Med. Chem. Lett. (2016) 7: 306-311 [PMID:26985320]
EP2 receptor/Prostanoid EP2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2488] [GtoPdb: 341] [UniProtKB: Q62053]
ChEMBL Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting B 7.66 pKi 22 nM Ki Bioorg. Med. Chem. Lett. (2012) 22: 396-401 [PMID:22119471]
ChEMBL Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting B 7.66 pKi 22 nM Ki Bioorg. Med. Chem. (2012) 20: 2235-2251 [PMID:22386979]
GtoPdb - - 7.9 pKi - - - Br J Pharmacol (1997) 122: 217-24 [PMID:9313928];
Endocrinology (2000) 141: 1554-9 [PMID:10746663];
Life Sci (2003) 74: 135-41 [PMID:14607240]
EP2 receptor/Prostanoid EP2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4909] [GtoPdb: 341] [UniProtKB: Q62928]
GtoPdb - - 8.2 pKi - - - Eur J Pharmacol (1997) 340: 227-41 [PMID:9537820]
ChEMBL Inhibition of rat EP2 receptor expressed in HEK293 cells B 8.28 pIC50 5.2 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 2075-2078 [PMID:19250823]
ChEMBL Agonist activity at rat EP2 receptor F 7.72 pEC50 19 nM EC50 Bioorg. Med. Chem. (2012) 20: 2235-2251 [PMID:22386979]
ChEMBL Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release F 9.7 pEC50 0.2 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 2075-2078 [PMID:19250823]
EP3 receptor/Prostanoid EP3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115]
GtoPdb - - 8.68 pKd 2.1 nM Kd Am J Physiol Renal Physiol (2008) 295: F984-94 [PMID:18632791]
GtoPdb - - 9.1 pKd 0.8 nM Kd Br J Pharmacol (2006) 148: 326-39 [PMID:16604093];
Biochem Pharmacol (2012) 84: 68-75 [PMID:22480736];
Am J Physiol Renal Physiol (2008) 295: F984-94 [PMID:18632791]
ChEMBL Binding affinity to EP3 receptor (unknown origin) B 8.3 pKi 5 nM Ki J. Med. Chem. (2014) 57: 4454-4465 [PMID:24279689]
ChEMBL Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method B 8.66 pKi 2.17 nM Ki J Med Chem (2019) 62: 4731-4741 [PMID:30964292]
GtoPdb - - 9.48 pKi 0.33 nM Ki Biochim Biophys Acta (2000) 1483: 285-93 [PMID:10634944]
ChEMBL Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells B 9.48 pKi 0.33 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 4323-4327 [PMID:17531488]
ChEMBL Displacement of [3H]PGE2 from human EP3 receptor B 9.48 pKi 0.33 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 821-824 [PMID:18039575]
ChEMBL Binding affinity to EP3 receptor B 9.03 pIC50 0.94 nM IC50 J. Med. Chem. (2010) 53: 4332-4353 [PMID:20218623]
ChEMBL Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis B 8.6 pEC50 2.5 nM EC50 ACS Med. Chem. Lett. (2016) 7: 306-311 [PMID:26985320]
EP3 receptor/Prostanoid EP3 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4336] [GtoPdb: 342] [UniProtKB: P30557]
GtoPdb - - 8.85 pKd 1.4 nM Kd Br J Pharmacol (1997) 122: 217-24 [PMID:9313928]
ChEMBL Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting B 8.3 pKi 5 nM Ki Bioorg. Med. Chem. Lett. (2012) 22: 396-401 [PMID:22119471]
ChEMBL Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting B 8.3 pKi 5 nM Ki Bioorg. Med. Chem. (2012) 20: 2235-2251 [PMID:22386979]
GtoPdb - - 9.07 pKi 0.85 nM Ki Br J Pharmacol (1997) 122: 217-24 [PMID:9313928]
EP3 receptor in Rat [GtoPdb: 342] [UniProtKB: P34980]
GtoPdb - - 8.41 pKd 3.9 nM Kd FEBS Lett (1994) 351: 119-22 [PMID:8076679];
Br J Pharmacol (2005) 145: 1132-42 [PMID:15937517]
GtoPdb - - 8.96 pKd 1.1 nM Kd Am J Physiol Renal Physiol (2008) 295: F984-94 [PMID:18632791]
GtoPdb - - 9.1 pKd 0.8 nM Kd Eur J Pharmacol (1997) 340: 227-41 [PMID:9537820];
Br J Pharmacol (2005) 145: 1132-42 [PMID:15937517];
Am J Physiol Renal Physiol (2008) 295: F984-94 [PMID:18632791]
GtoPdb - - 9 pKi - - - Eur J Pharmacol (1997) 340: 227-41 [PMID:9537820]
GtoPdb - - 9.39 pEC50 0.41 nM EC50 Eur J Pharmacol (1997) 340: 227-41 [PMID:9537820]
EP4 receptor/Prostanoid EP4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408]
ChEMBL Binding affinity to EP4 receptor (unknown origin) B 8.51 pKi 3.1 nM Ki J. Med. Chem. (2014) 57: 4454-4465 [PMID:24279689]
ChEMBL Displacement of radiolabeled PGE2 from human prostanoid EP4 receptor B 8.72 pKi 1.9 nM Ki J. Med. Chem. (2008) 51: 7094-7098 [PMID:18983139]
GtoPdb - - 9.1 pKi 0.79 nM Ki Br J Pharmacol (2006) 148: 326-39 [PMID:16604093];
Biochim Biophys Acta (2000) 1483: 285-93 [PMID:10634944];
Mol Pharmacol (1999) 56: 545-51 [PMID:10462542];
Br J Pharmacol (2000) 130: 1919-1926 [PMID:10952683];
J Pharmacol Exp Ther (2007) 322: 686-94 [PMID:17495127]
ChEMBL Binding affinity at human prostaglandin EP4 receptor B 9.1 pKi 0.79 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 6572-6575 [PMID:17931866]
ChEMBL Displacement of [3H]PGE4 from human EP4 receptor B 9.1 pKi 0.79 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 821-824 [PMID:18039575]
ChEMBL Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells B 9.1 pKi 0.79 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 4323-4327 [PMID:17531488]
ChEMBL Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs B 9.35 pKi 0.45 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Binding affinity to human prostanoid EP4 receptor by radioligand displacement assay B 9.77 pKi 0.17 nM Ki Eur. J. Med. Chem. (2013) 63: 85-94 [PMID:23466604]
ChEMBL Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method B 9.96 pKi 0.11 nM Ki J Med Chem (2019) 62: 4731-4741 [PMID:30964292]
ChEMBL Binding affinity to EP4 receptor B 8 pIC50 9.9 nM IC50 J. Med. Chem. (2010) 53: 4332-4353 [PMID:20218623]
ChEMBL Displacement of radiolabeled PGE2 from human prostanoid EP4 receptor B 8.42 pIC50 3.8 nM IC50 J. Med. Chem. (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs B 8.96 pIC50 1.1 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Inhibitory activity against human EP4 receptor expressed in HEK293 ebna cells B 9.15 pIC50 0.7 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 1129-1132 [PMID:12643927]
ChEMBL Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method B 9.26 pIC50 0.55 nM IC50 Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]
ChEMBL Binding affinity to human prostanoid EP4 receptor by radioligand displacement assay B 9.35 pIC50 0.45 nM IC50 Eur. J. Med. Chem. (2013) 63: 85-94 [PMID:23466604]
GtoPdb - - 6.05 pEC50 900 nM EC50 J Pharmacol Exp Ther (2009) 331: 297-307 [PMID:19584306]
ChEMBL Agonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method B 8.12 pEC50 7.5 nM EC50 ACS Med. Chem. Lett. (2016) 7: 306-311 [PMID:26985320]
ChEMBL EP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 receptor F 8.52 pEC50 3 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 1129-1132 [PMID:12643927]
ChEMBL Agonist activity at human EP4 receptor by cAMP assay F 8.52 pEC50 3 nM EC50 Bioorg. Med. Chem. Lett. (2008) 18: 821-824 [PMID:18039575]
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 B 9.23 pEC50 0.58 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 B 10.7 pEC50 0.02 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 - - 8.6 pKd 2.5 nM Kd Br J Pharmacol (1997) 122: 217-24 [PMID:9313928]
ChEMBL Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation counting B 8.51 pKi 3.1 nM Ki Bioorg. Med. Chem. Lett. (2012) 22: 396-401 [PMID:22119471]
ChEMBL Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting B 8.51 pKi 3.1 nM Ki Bioorg. Med. Chem. (2012) 20: 2235-2251 [PMID:22386979]
GtoPdb - - 8.7 pKi 2 nM Ki Br J Pharmacol (1997) 122: 217-24 [PMID:9313928];
Endocrinology (2000) 141: 1554-9 [PMID:10746663]
EP4 receptor/Prostanoid EP4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4086] [GtoPdb: 343] [UniProtKB: P43114]
GtoPdb - - 9 pKi - - - Eur J Pharmacol (1997) 340: 227-41 [PMID:9537820]
ChEMBL Inhibition of rat EP4 receptor expressed in HEK293 cells B 8.68 pIC50 2.1 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 2075-2078 [PMID:19250823]
ChEMBL Agonist activity at rat EP4 receptor F 8.46 pEC50 3.5 nM EC50 Bioorg. Med. Chem. (2012) 20: 2235-2251 [PMID:22386979]
ChEMBL Agonist activity against rat EP4 receptor expressed in HEK293 cells assessed as stimulation of cAMP release F 9.15 pEC50 0.7 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 2075-2078 [PMID:19250823]
FP receptor/Prostanoid FP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1987] [GtoPdb: 344] [UniProtKB: P43088]
GtoPdb - - 6.9 pKi - - - Biochim Biophys Acta (2000) 1483: 285-93 [PMID:10634944];
Biochem J (2003) 371: 443-9 [PMID:12519077]
ChEMBL Agonist activity at human FP receptor expressed in human Chem1 cells assessed as increase in intracellular calcium level by fluorescence based analysis B 6.6 pEC50 250 nM EC50 ACS Med. Chem. Lett. (2016) 7: 306-311 [PMID:26985320]
FP receptor in Mouse [GtoPdb: 344] [UniProtKB: P43117]
GtoPdb - - 7 pKi - - - Br J Pharmacol (1997) 122: 217-24 [PMID:9313928]
IP receptor/Prostanoid IP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119]
ChEMBL Binding affinity to prostanoid IP receptor (unknown origin) B 5 pKi >10000 nM Ki J. Med. Chem. (2014) 57: 4454-4465 [PMID:24279689]
ChEMBL Agonist activity at prostanoid IP receptor (unknown origin) by functional assay B 6.59 pIC50 260 nM IC50 J. Med. Chem. (2014) 57: 4454-4465 [PMID:24279689]
ChEMBL Agonist activity at human IP receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method B 6.46 pEC50 347 nM EC50 ACS Med. Chem. Lett. (2016) 7: 306-311 [PMID:26985320]
OAT6/Solute carrier family 22 member 20 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5269] [GtoPdb: 1037] [UniProtKB: Q80UJ1]
ChEMBL Inhibition of mouse Oat6-mediated [3H]ES uptake in Xenopus oocytes after 1 hr B 4.74 pKi 18197.01 nM Ki J. Biol. Chem. (2007) 282: 23841-23853 [PMID:17553798]
ChEMBL Inhibition of mouse Oat6-mediated [3H]ES uptake in Xenopus oocytes after 1 hr B 4.74 pKi 18000 nM Ki J. Biol. Chem. (2007) 282: 23841-23853 [PMID:17553798]
Organic anion transporter 1/Solute carrier family 22 member 6 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5653] [GtoPdb: 1025] [UniProtKB: Q8VC69]
ChEMBL Inhibition of mouse Oat1-mediated [3H]PAH uptake in Xenopus oocytes after 1 hr B 5.47 pKi 3400 nM Ki J. Biol. Chem. (2007) 282: 23841-23853 [PMID:17553798]
ChEMBL Inhibition of mouse Oat1-mediated [3H]PAH uptake in Xenopus oocytes after 1 hr B 5.47 pKi 3388.44 nM Ki J. Biol. Chem. (2007) 282: 23841-23853 [PMID:17553798]
DP1 receptor in Human [GtoPdb: 338] [UniProtKB: Q13258]
GtoPdb - - 7 pKi - - - J Biol Chem (1995) 270: 18910-6 [PMID:7642548];
Br J Pharmacol (1998) 123: 1317-24 [PMID:9579725];
Biochim Biophys Acta (2000) 1483: 285-93 [PMID:10634944]
DP2 receptor in Human [GtoPdb: 339] [UniProtKB: Q9Y5Y4]
GtoPdb - - 5.3 pKi - - - Br J Pharmacol (2002) 137: 1163-72 [PMID:12466225]
DP2 receptor in Mouse [GtoPdb: 339] [UniProtKB: Q9Z2J6]
GtoPdb - - 5.5 pKi - - - J Pharmacol Exp Ther (2003) 306: 463-70 [PMID:12721327]
TP receptor in Human [GtoPdb: 346] [UniProtKB: P21731]
GtoPdb - - 4.5 pKi - - - Biochim Biophys Acta (2000) 1483: 285-93 [PMID:10634944]
CatSper1 in Human [GtoPdb: 388] [UniProtKB: Q8NEC5]
GtoPdb Patch clamp electrophysiology - 6.3 pEC50 500 nM EC50 Nature (2011) 471: 387-91 [PMID:21412339]
CatSper2 in Human [GtoPdb: 389] [UniProtKB: Q96P56]