PGF [Ligand Id: 1884] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL815 (U-14583, Dinoprost, U-14,583)
  • DP1 receptor/Prostanoid DP receptor in Human [ChEMBL: CHEMBL4427] [GtoPdb: 338] [UniProtKB: Q13258]
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  • EP1 receptor/Prostanoid EP1 receptor in Human [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995]
  • EP1 receptor in Mouse [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 in Rat [GtoPdb: 341] [UniProtKB: Q62928]
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  • EP3 receptor/Prostanoid EP3 receptor in Human [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115]
  • EP3 receptor in Mouse [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 in Rat [GtoPdb: 343] [UniProtKB: P43114]
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  • FP receptor/Prostanoid FP receptor in Human [ChEMBL: CHEMBL1987] [GtoPdb: 344] [UniProtKB: P43088]
  • Prostanoid FP receptor in Bovine [ChEMBL: CHEMBL4820] [UniProtKB: P37289]
  • FP receptor/Prostanoid FP receptor in Mouse [ChEMBL: CHEMBL5000] [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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  • OATP2A1/Solute carrier organic anion transporter family member 2A1 in Human [ChEMBL: CHEMBL2073703] [GtoPdb: 1223] [UniProtKB: Q92959]
  • OATP2A1/Solute carrier organic anion transporter family member 2A1 in Mouse [ChEMBL: CHEMBL2073699] [GtoPdb: 1223] [UniProtKB: Q9EPT5]
  • OATP2A1/Solute carrier organic anion transporter family member 2A1 in Rat [ChEMBL: CHEMBL2073680] [GtoPdb: 1223] [UniProtKB: Q00910]
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  • OATP2B1/Solute carrier organic anion transporter family member 2B1 in Rat [ChEMBL: CHEMBL2073698] [GtoPdb: 1224] [UniProtKB: Q9JHI3]
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  • TP receptor/Thromboxane A2 receptor in Human [ChEMBL: CHEMBL2069] [GtoPdb: 346] [UniProtKB: P21731]
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  • DP2 receptor in Human [GtoPdb: 339] [UniProtKB: Q9Y5Y4]
  • DP2 receptor in Mouse [GtoPdb: 339] [UniProtKB: Q9Z2J6]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
DP1 receptor/Prostanoid DP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4427] [GtoPdb: 338] [UniProtKB: Q13258]
GtoPdb - - 6.4 pKi - - - Br J Pharmacol (1998) 123: 1317-24 [PMID:9579725];
Biochim Biophys Acta (2000) 1483: 285-93 [PMID:10634944]
ChEMBL Affinity for human Prostaglandin D2 receptor expressed in HEK293 cells B 5.35 pIC50 4500 nM IC50 J. Med. Chem. (2000) 43: 945-952 [PMID:10715159]
ChEMBL In vitro binding at DP human prostaglandin receptor using [3H]- PGD-2 as radioligand B 5.35 pIC50 4500 nM IC50 J. Med. Chem. (2001) 44: 4157-4169 [PMID:11708917]
EP1 receptor/Prostanoid EP1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995]
GtoPdb - - 6.3 pKi - - - Biochim Biophys Acta (2000) 1483: 285-93 [PMID:10634944];
J Pharm Pharmacol (2002) 54: 539-47 [PMID:11999132]
ChEMBL Affinity for Prostanoid EP1 receptor expressed in COS-7 cells. B 6.42 pIC50 380 nM IC50 J. Med. Chem. (2000) 43: 945-952 [PMID:10715159]
ChEMBL In vitro binding at EP1 human prostaglandin receptor using [3H]PGE-2 as radioligand B 6.66 pIC50 220 nM IC50 J. Med. Chem. (2001) 44: 4157-4169 [PMID:11708917]
ChEMBL Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP1 (% of control ligand, 17-phi-PGE2=80%) F 6.22 pEC50 600 nM EC50 Bioorg. Med. Chem. Lett. (2000) 10: 1519-1522 [PMID:10915040]
EP1 receptor in Mouse [GtoPdb: 340] [UniProtKB: P35375]
GtoPdb - - 5.9 pKi - - - Br J Pharmacol (1997) 122: 217-24 [PMID:9313928]
EP1 receptor in Rat [GtoPdb: 340] [UniProtKB: P70597]
GtoPdb - - 6.4 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]
GtoPdb - - 6 pKi - - - Biochim Biophys Acta (2000) 1483: 285-93 [PMID:10634944];
Mol Pharmacol (1999) 56: 545-51 [PMID:10462542]
ChEMBL In vitro binding at EP2 human prostaglandin receptor using [3H]PGE-2 as radioligand B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2001) 44: 4157-4169 [PMID:11708917]
ChEMBL Affinity for Prostanoid EP2 receptor expressed in CHO cells B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2000) 43: 945-952 [PMID:10715159]
EP2 receptor in Rat [GtoPdb: 341] [UniProtKB: Q62928]
GtoPdb - - 5.6 pKi - - - Eur J Pharmacol (1997) 340: 227-41 [PMID:9537820]
EP3 receptor/Prostanoid EP3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115]
GtoPdb - - 7.42 pKi 38 nM Ki Biochim Biophys Acta (2000) 1483: 285-93 [PMID:10634944]
ChEMBL Affinity for Prostanoid EP3 receptor expressed in CHO cell line B 6.49 pIC50 322 nM IC50 J. Med. Chem. (2000) 43: 945-952 [PMID:10715159]
ChEMBL In vitro binding at EP3 human prostaglandin receptor using [3H]PGE-2 as radioligand B 6.96 pIC50 110 nM IC50 J. Med. Chem. (2001) 44: 4157-4169 [PMID:11708917]
ChEMBL Functional activity in RAT-1cells, transiently-transfected with human Prostaglandin E receptor EP3 (% of control ligand, sulprostone=50%) F 5.64 pEC50 2300 nM EC50 Bioorg. Med. Chem. Lett. (2000) 10: 1519-1522 [PMID:10915040]
EP3 receptor in Mouse [GtoPdb: 342] [UniProtKB: P30557]
GtoPdb - - 7.12 pKi 75 nM Ki Br J Pharmacol (1997) 122: 217-24 [PMID:9313928]
EP3 receptor in Rat [GtoPdb: 342] [UniProtKB: P34980]
GtoPdb - - 6.67 pKi 213 nM Ki Eur J Pharmacol (1997) 340: 227-41 [PMID:9537820]
GtoPdb - - 8.38 pEC50 4.2 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]
GtoPdb - - 9.49 pKi 0.32 nM Ki 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]
ChEMBL Affinity for Prostanoid EP4 receptor expressed in CHO cells B 5.38 pIC50 4200 nM IC50 J. Med. Chem. (2000) 43: 945-952 [PMID:10715159]
ChEMBL In vitro binding at EP4 human prostaglandin receptor using [3H]PGE-2 as radioligand B 5.38 pIC50 4200 nM IC50 J. Med. Chem. (2001) 44: 4157-4169 [PMID:11708917]
GtoPdb - - 6.05 pEC50 900 nM EC50 J Pharmacol Exp Ther (2009) 331: 297-307 [PMID:19584306]
EP4 receptor in Rat [GtoPdb: 343] [UniProtKB: P43114]
GtoPdb - - 6.2 pKi - - - Eur J Pharmacol (1997) 340: 227-41 [PMID:9537820]
FP receptor/Prostanoid FP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1987] [GtoPdb: 344] [UniProtKB: P43088]
ChEMBL Inhibitory Binding constant (n=2) to Prostanoid FP receptor expressed in bovine corpus luteum B 6.92 pKi 119 nM Ki J. Med. Chem. (2000) 43: 3400-3407 [PMID:10978187]
GtoPdb - - 8.5 pKi - - - Br J Pharmacol (2006) 148: 326-39 [PMID:16604093];
Biochim Biophys Acta (2000) 1483: 285-93 [PMID:10634944];
Biochem J (2003) 371: 443-9 [PMID:12519077]
ChEMBL Binding potency towards Prostaglandin F2 alpha receptor (competitive binding) with natural [3H]-PGF 2 alpha in ovine luteal cells (OLC) B 7.37 pIC50 43 nM IC50 J. Med. Chem. (1989) 32: 256-264 [PMID:2909739]
ChEMBL Affinity for human Prostanoid FP receptor expressed in COS-7 cells B 8.15 pIC50 7 nM IC50 J. Med. Chem. (2000) 43: 945-952 [PMID:10715159]
ChEMBL In vitro binding at FP human prostaglandin receptor using [3H]PGF-2 alpha as radioligand B 8.52 pIC50 3 nM IC50 J. Med. Chem. (2001) 44: 4157-4169 [PMID:11708917]
ChEMBL Displacement of [3H]PGF2-alpha from human FP-receptor expressed in CHO-KI cells B 8.6 pIC50 2.5 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 1519-1522 [PMID:10915040]
ChEMBL Functional activity in RAT-1cells, transiently-transfected with human FP-receptor (% of control ligand, fluprostenol=75%) F 7.1 pEC50 79 nM EC50 Bioorg. Med. Chem. Lett. (2000) 10: 1519-1522 [PMID:10915040]
ChEMBL Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cells F 7.61 pEC50 24.5 nM EC50 Bioorg. Med. Chem. Lett. (2004) 14: 4525-4528 [PMID:15357985]
Prostanoid FP receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4820] [UniProtKB: P37289]
ChEMBL Displacement of [3H]PGF2 alpha from FP receptor in bovine corpus luteum membrane B 6.89 pKi 130 nM Ki Bioorg. Med. Chem. (2009) 17: 576-584 [PMID:19101156]
ChEMBL Binding affinity for Prostanoid FP receptor of bovine corpus luteum B 6.89 pKi 129 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 4525-4528 [PMID:15357985]
ChEMBL Binding potency towards Prostaglandin F2 alpha receptor (competitive binding) with natural [3H]-PGF 2 alpha in bovine corpora lutea plasma membranes (BCLM) B 6.85 pIC50 140 nM IC50 J. Med. Chem. (1989) 32: 256-264 [PMID:2909739]
FP receptor/Prostanoid FP receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5000] [GtoPdb: 344] [UniProtKB: P43117]
GtoPdb - - 8.5 pKi - - - Br J Pharmacol (1997) 122: 217-24 [PMID:9313928]
ChEMBL Agonist activity at FP receptor in Swiss mouse 3T3 cells assessed as [3H]-IP accumulation by scintillation counting F 7.61 pEC50 24.5 nM EC50 Bioorg. Med. Chem. (2009) 17: 576-584 [PMID:19101156]
ChEMBL Agonist activity at FP receptor in mouse 3T3 fibroblast cells assessed as intracellular calcium mobilization by FLIPR F 7.9 pEC50 12.59 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 939-943 [PMID:23317571]
IP receptor/Prostanoid IP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119]
ChEMBL In vitro binding at prostanoid IP receptor using [3H]iloprost as radioligand B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2001) 44: 4157-4169 [PMID:11708917]
ChEMBL Affinity for Prostaglandin I2 receptor expressed in CHO cells B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2000) 43: 945-952 [PMID:10715159]
OATP2A1/Solute carrier organic anion transporter family member 2A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073703] [GtoPdb: 1223] [UniProtKB: Q92959]
ChEMBL TP_TRANSPORTER: inhibition of PGE2 uptake in PGT-expressing HeLa cells F 7.64 pKi 23 nM Ki Am. J. Physiol. (1999) 277: R734-R741 [PMID:10484490]
OATP2A1/Solute carrier organic anion transporter family member 2A1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073699] [GtoPdb: 1223] [UniProtKB: Q9EPT5]
ChEMBL TP_TRANSPORTER: inhibition of PGE2 uptake in PGT-expressing HeLa cells F 6.98 pKi 104 nM Ki Am. J. Physiol. (1999) 277: R734-R741 [PMID:10484490]
OATP2A1/Solute carrier organic anion transporter family member 2A1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073680] [GtoPdb: 1223] [UniProtKB: Q00910]
ChEMBL TP_TRANSPORTER: inhibition of PGE2 uptake in PGT-expressing HeLa cells F 7.35 pKi 45 nM Ki Am. J. Physiol. (1999) 277: R734-R741 [PMID:10484490]
OATP2B1/Solute carrier organic anion transporter family member 2B1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073698] [GtoPdb: 1224] [UniProtKB: Q9JHI3]
ChEMBL TP_TRANSPORTER: inhibition of PGD2 uptake in Xenopus laevis oocytes F 6.54 pIC50 287 nM IC50 Biochem. Biophys. Res. Commun. (2000) 275: 831-838 [PMID:10973807]
TP receptor/Thromboxane A2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069] [GtoPdb: 346] [UniProtKB: P21731]
GtoPdb - - 5.1 pKi - - - Biochim Biophys Acta (2000) 1483: 285-93 [PMID:10634944]
ChEMBL Affinity for Prostanoid TP receptor expressed in CHO cells B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2000) 43: 945-952 [PMID:10715159]
ChEMBL Functional activity in RAT-1cells, transiently-transfected with human TP-receptor (% of control ligand, [3H]-U-46,619=95%) F 5.85 pEC50 1400 nM EC50 Bioorg. Med. Chem. Lett. (2000) 10: 1519-1522 [PMID:10915040]
DP2 receptor in Human [GtoPdb: 339] [UniProtKB: Q9Y5Y4]
GtoPdb - - 6.4 pKi - - - Br J Pharmacol (2002) 137: 1163-72 [PMID:12466225]
DP2 receptor in Mouse [GtoPdb: 339] [UniProtKB: Q9Z2J6]
GtoPdb - - 6.2 pKi - - - J Pharmacol Exp Ther (2003) 306: 463-70 [PMID:12721327]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]