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ChEMBL ligand: CHEMBL548 (Cervidil, Dinoprostona, Dinoprostone, Dinoprostone beta-cyclodextrin clathrate, Enzaprost e, Minprostin e2, NSC-165560, NSC-196514, Prepidil, Propess, Prostaglandin e2, Prostin e2, U-12,062, U-12062) |
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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] | ||||||||
GtoPdb | - | - | 7.9 | pKd | 1 | nM | Kd |
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 | Binding affinity to EP1 receptor (unknown origin) | B | 7.74 | pKi | 18 | nM | Ki | J Med Chem (2014) 57: 4454-4465 [PMID:24279689] |
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 | F | 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] | ||||||||
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 | - | - | 7.6 | pKd | - | - | - |
J Biol Chem (1996) 271: 31255-61 [PMID:8940129]; 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] | ||||||||
GtoPdb | - | - | 7.9 | pKd | 12.5 | nM | Kd |
Br J Pharmacol (2006) 148: 326-39 [PMID:16604093]; Biochim Biophys Acta (2000) 1483: 285-93 [PMID:10634944] |
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] |
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 | F | 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 | F | 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 | F | 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] | ||||||||
GtoPdb | - | - | 7.7 | pKd | - | - | - | J Biol Chem (2004) 279: 11016-26 [PMID:14699136] |
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] |
EP2 receptor/Prostanoid EP2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4909] [GtoPdb: 341] [UniProtKB: Q62928] | ||||||||
GtoPdb | - | - | 8.3 | pKd | - | - | - |
Eur J Pharmacol (1997) 340: 227-41 [PMID:9537820]; Prostaglandins (1997) 54: 713-25 [PMID:9440134] |
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 | - | - | 9.5 | pKd | 0.3 | nM | Kd |
Br J Pharmacol (2006) 148: 326-39 [PMID:16604093]; Biochim Biophys Acta (2000) 1483: 285-93 [PMID:10634944] |
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] |
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 | F | 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] | ||||||||
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] |
EP3 receptor in Rat [GtoPdb: 342] [UniProtKB: P34980] | ||||||||
GtoPdb | - | - | 9.1 | pKd | - | - | - | 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] | ||||||||
GtoPdb | - | - | 9.52 | pKd | 0.3 | nM | Kd |
Br J Pharmacol (2006) 148: 326-39 [PMID:16604093]; Biochim Biophys Acta (2000) 1483: 285-93 [PMID:10634944]; Br J Pharmacol (2000) 130: 1919-1926 [PMID:10952683]; Biochem Pharmacol (2012) 84: 68-75 [PMID:22480736] |
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] |
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] |
ChEMBL | Agonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method | F | 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 | F | 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 | F | 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] | ||||||||
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] |
EP4 receptor/Prostanoid EP4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4086] [GtoPdb: 343] [UniProtKB: P43114] | ||||||||
GtoPdb | - | - | 9 | pKd | - | - | - | 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] | ||||||||
ChEMBL | Agonist activity at human FP receptor expressed in human Chem1 cells assessed as increase in intracellular calcium level by fluorescence based analysis | F | 6.6 | pEC50 | 250 | nM | EC50 | ACS Med Chem Lett (2016) 7: 306-311 [PMID:26985320] |
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 | F | 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] |
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]