PGF2α [Ligand Id: 1884] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL815 (Dinoprost, Pgf2a, Pgf2alpha, Prosmon, Prostaglandin f2-alpha, Prostaglandin f2.alpha., Prostaglandin f2alpha, U-14,583, U-14583) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 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]
