PGF2α [Ligand Id: 1884] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL815 (Dinoprost, Pgf2a, Pgf2alpha, Prosmon, Prostaglandin f2-alpha, Prostaglandin f2.alpha., Prostaglandin f2alpha, U-14,583, U-14583) |
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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 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]
