PGE2 [Ligand Id: 1883] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL548 (Cervidil, 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] | ||||||||
| 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 | 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] | ||||||||
| 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 | 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] | ||||||||
| 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 | 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] | ||||||||
| 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 | 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] | ||||||||
| 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 | F | 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 | 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] |
| 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] |