PGE1 [Ligand Id: 1882] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL495 (Alprostadil, Caverject, Caverject impulse, Edex, NSC-165559, ONO-1608, Pge1, Prostaglandin e1, Prostin, Prostin vr, Prostin vr pediatric, U-10,136, U-10136, Viridal 10, Viridal 20, Viridal 5, Viridal duo, Vitaros) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| EP1 receptor in Human [GtoPdb: 340] [UniProtKB: P34995] | ||||||||
| GtoPdb | - | - | 6.8 | pKi | - | - | - | J Pharm Pharmacol (2002) 54: 539-47 [PMID:11999132] |
| EP1 receptor/Prostanoid EP1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2181] [GtoPdb: 340] [UniProtKB: P35375] | ||||||||
| ChEMBL | Binding affinity towards mouse Prostanoid EP1 receptor in CHO cells. | B | 7 | pKi | 100 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2025-2028 [PMID:11454472] |
| GtoPdb | - | - | 7.4 | pKi | - | - | - | Br J Pharmacol (1997) 122: 217-24 [PMID:9313928] |
| ChEMBL | Evaluated for its competitive binding affinity towards mouse Prostanoid EP1 receptor in CHO cells expressing prostanoid receptor | B | 7.66 | pKi | 22 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2029-2031 [PMID:11454473] |
| ChEMBL | Affinity for mouse Prostanoid EP1 receptor expressed in CHO cells | B | 7.66 | pKi | 22 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2033-2035 [PMID:11454474] |
| ChEMBL | Affinity for mouse Prostanoid EP1 receptor expressed in CHO cells | B | 8.22 | pKi | 6 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2033-2035 [PMID:11454474] |
| EP1 receptor in Rat [GtoPdb: 340] [UniProtKB: P70597] | ||||||||
| GtoPdb | - | - | 7 | pKi | - | - | - | Eur J Pharmacol (1997) 340: 227-41 [PMID:9537820] |
| EP2 receptor in Human [GtoPdb: 341] [UniProtKB: P43116] | ||||||||
| GtoPdb | - | - | 8.04 | pKi | 9.1 | nM | Ki | J Biol Chem (1994) 269: 11873-7 [PMID:8163486] |
| EP2 receptor/Prostanoid EP2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2488] [GtoPdb: 341] [UniProtKB: Q62053] | ||||||||
| ChEMBL | Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells. | B | 7.06 | pKi | 87 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2025-2028 [PMID:11454472] |
| ChEMBL | Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor | B | 7.39 | pKi | 41 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2029-2031 [PMID:11454473] |
| ChEMBL | Affinity for mouse Prostanoid EP2 receptor expressed in CHO cells | B | 7.39 | pKi | 41 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2033-2035 [PMID:11454474] |
| ChEMBL | Affinity for mouse Prostanoid EP2 receptor expressed in CHO cells | B | 7.66 | pKi | 22 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2033-2035 [PMID:11454474] |
| GtoPdb | - | - | 8 | pKi | - | - | - | Br J Pharmacol (1997) 122: 217-24 [PMID:9313928] |
| ChEMBL | Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor | F | 8.59 | pEC50 | 2.6 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 2025-2028 [PMID:11454472] |
| EP2 receptor in Rat [GtoPdb: 341] [UniProtKB: Q62928] | ||||||||
| GtoPdb | - | - | 8 | pKi | - | - | - | Eur J Pharmacol (1997) 340: 227-41 [PMID:9537820] |
| EP3 receptor/Prostanoid EP3 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4336] [GtoPdb: 342] [UniProtKB: P30557] | ||||||||
| ChEMBL | Binding affinity towards mouse Prostanoid EP3 receptor in CHO cells. | B | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2025-2028 [PMID:11454472] |
| ChEMBL | Evaluated for its competitive binding affinity towards mouse Prostanoid EP3 receptor in CHO cells expressing prostanoid receptor | B | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2029-2031 [PMID:11454473] |
| ChEMBL | Affinity for mouse Prostanoid EP3 receptor expressed in CHO cells | B | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2033-2035 [PMID:11454474] |
| ChEMBL | Affinity for mouse Prostanoid EP3 receptor expressed in CHO cells | B | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2033-2035 [PMID:11454474] |
| GtoPdb | - | - | 9 | pKi | 1 | nM | Ki | Br J Pharmacol (1997) 122: 217-24 [PMID:9313928] |
| EP3 receptor in Rat [GtoPdb: 342] [UniProtKB: P34980] | ||||||||
| GtoPdb | - | - | 9 | pKi | 1 | nM | Ki | Eur J Pharmacol (1997) 340: 227-41 [PMID:9537820] |
| GtoPdb | - | - | 9.35 | pEC50 | 0.45 | nM | EC50 | Eur J Pharmacol (1997) 340: 227-41 [PMID:9537820] |
| EP4 receptor in Human [GtoPdb: 343] [UniProtKB: P35408] | ||||||||
| GtoPdb | - | - | 8.8 | pKi | 1.58 | nM | Ki | Br J Pharmacol (2000) 130: 1919-1926 [PMID:10952683] |
| GtoPdb | - | - | 9.51 | pEC50 | 0.31 | nM | EC50 | J Pharmacol Exp Ther (2009) 331: 297-307 [PMID:19584306] |
| EP4 receptor/Prostanoid EP4 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2489] [GtoPdb: 343] [UniProtKB: P32240] | ||||||||
| ChEMBL | Binding affinity towards mouse Prostanoid EP4 receptor in CHO cells. | B | 8.48 | pKi | 3.3 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2025-2028 [PMID:11454472] |
| ChEMBL | Evaluated for its competitive binding affinity towards mouse Prostanoid EP4 receptor in CHO cells expressing prostanoid receptor | B | 8.48 | pKi | 3.3 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2029-2031 [PMID:11454473] |
| ChEMBL | Affinity for mouse Prostanoid EP4 receptor expressed in CHO cells | B | 8.48 | pKi | 3.3 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2033-2035 [PMID:11454474] |
| ChEMBL | Affinity for mouse Prostanoid EP4 receptor expressed in CHO cells | B | 8.51 | pKi | 3.1 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2033-2035 [PMID:11454474] |
| GtoPdb | - | - | 8.7 | pKi | - | - | - | Br J Pharmacol (1997) 122: 217-24 [PMID:9313928] |
| ChEMBL | Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor | F | 8.44 | pEC50 | 3.6 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 2033-2035 [PMID:11454474] |
| ChEMBL | Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP4 receptor | F | 8.6 | pEC50 | 2.5 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 2029-2031 [PMID:11454473] |
| ChEMBL | Effective concentration for increased intracellular c-AMP production by mouse Prostanoid EP4 receptor | F | 8.6 | pEC50 | 2.5 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 2033-2035 [PMID:11454474] |
| EP4 receptor in Rat [GtoPdb: 343] [UniProtKB: P43114] | ||||||||
| GtoPdb | - | - | 9.2 | pKi | - | - | - | Eur J Pharmacol (1997) 340: 227-41 [PMID:9537820] |
| IP receptor/Prostanoid IP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119] | ||||||||
| ChEMBL | Affinity for human Prostanoid IP receptor expressed in CHO cells | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2033-2035 [PMID:11454474] |
| GtoPdb | - | - | 6.82 | pKi | 150 | nM | Ki |
Bioorg Med Chem Lett (2001) 11: 2029-31 [PMID:11454473]; Br J Pharmacol (2007) 152: 513-22 [PMID:17704830] |
| ChEMBL | Binding affinity towards human Prostanoid IP receptor in CHO cells. | B | 6.82 | pKi | 150 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2025-2028 [PMID:11454472] |
| ChEMBL | Evaluated for its competitive binding affinity towards human Prostanoid IP receptor in CHO cells | B | 6.82 | pKi | 150 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2029-2031 [PMID:11454473] |
| ChEMBL | Affinity for human Prostanoid IP receptor expressed in CHO cells | B | 6.82 | pKi | 150 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2033-2035 [PMID:11454474] |
| ChEMBL | Displacement of [3H]iloprost from Prostaglandin I2 receptor of human platelets | B | 5.85 | pIC50 | 1400 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 1071-1076 |
| ChEMBL | Effective concentration which increases intracellular c-AMP production in human Prostanoid IP receptor | F | 8.74 | pEC50 | 1.8 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 2025-2028 [PMID:11454472] |
| IP receptor in Mouse [GtoPdb: 345] [UniProtKB: P43252] | ||||||||
| GtoPdb | - | - | 7.5 | pKi | - | - | - | Br J Pharmacol (1997) 122: 217-24 [PMID:9313928] |
| 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 | 7.45 | pIC50 | 35.8 | nM | IC50 | Biochem Biophys Res Commun (2000) 275: 831-838 [PMID:10973807] |
| DP1 receptor in Human [GtoPdb: 338] [UniProtKB: Q13258] | ||||||||
| GtoPdb | - | - | 7.3 | pKi | - | - | - | Br J Pharmacol (1998) 123: 1317-24 [PMID:9579725] |
| CatSper1 in Human [GtoPdb: 388] [UniProtKB: Q8NEC5] | ||||||||
| GtoPdb | Patch clamp electrophysiology | - | 6.3 | pEC50 | 500 | nM | EC50 | Nature (2011) 471: 387-91 [PMID:21412339] |
| CatSper2 in Human [GtoPdb: 389] [UniProtKB: Q96P56] | ||||||||
| GtoPdb | Patch clamp electrophysiology. | - | 6.3 | pEC50 | 500 | nM | EC50 | Nature (2011) 471: 387-91 [PMID:21412339] |
| CatSper3 in Human [GtoPdb: 390] [UniProtKB: Q86XQ3] | ||||||||
| GtoPdb | Patch clamp electrophysiology. | - | 6.3 | pEC50 | 500 | nM | EC50 | Nature (2011) 471: 387-91 [PMID:21412339] |
| CatSper4 in Human [GtoPdb: 391] [UniProtKB: Q7RTX7] | ||||||||
| GtoPdb | Patch clamp electrophysiology. | - | 6.3 | pEC50 | 500 | nM | EC50 | Nature (2011) 471: 387-91 [PMID:21412339] |
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]
