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 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 |
|---|---|---|---|---|---|---|---|---|
| Nuclear receptor related 1/Nuclear receptor subfamily 4 group A member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5002] [GtoPdb: 630] [UniProtKB: P43354] | ||||||||
| ChEMBL | Agonist activity at Nurr1 in human SK-N-BE(2)-C cells measured by NBRE-based luciferase reporter gene assay | B | 5.52 | pEC50 | 3000 | nM | EC50 | J Med Chem (2022) 65: 9548-9563 [PMID:35797147] |
| ChEMBL | Agonist activity at Nurr1 in human SK-N-BE(2)-C cells measured by Gal4-based luciferase reporter gene assay | B | 5.52 | pEC50 | 3000 | nM | EC50 | J Med Chem (2022) 65: 9548-9563 [PMID:35797147] |
| Nuclear receptor related 1/Nuclear receptor subfamily 4 group A member 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879839] [GtoPdb: 630] [UniProtKB: Q06219] | ||||||||
| ChEMBL | Agonist activity at Nurr1 in mouse MN9D cells measured by NBRE-based luciferase reporter gene assay | B | 5.52 | pEC50 | 3000 | nM | EC50 | J Med Chem (2022) 65: 9548-9563 [PMID:35797147] |
| ChEMBL | Agonist activity at Nurr1 in mouse MN9D cells measured by Gal4-based luciferase reporter gene assay | B | 5.52 | pEC50 | 3000 | nM | EC50 | J Med Chem (2022) 65: 9548-9563 [PMID:35797147] |
| Nuclear receptor related 1/Nuclear receptor subfamily 4 group A member 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523278] [GtoPdb: 630] [UniProtKB: Q07917] | ||||||||
| ChEMBL | Agonist activity at Nurr1 in rat N27-A cells measured by NBRE-based luciferase reporter gene assay | B | 5.52 | pEC50 | 3000 | nM | EC50 | J Med Chem (2022) 65: 9548-9563 [PMID:35797147] |
| ChEMBL | Agonist activity at Nurr1 in rat N27-A cells measured by Gal4-based luciferase reporter gene assay | B | 5.52 | pEC50 | 3000 | nM | EC50 | J Med Chem (2022) 65: 9548-9563 [PMID:35797147] |
| 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 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]
