PGE1 [Ligand Id: 1882] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL495 (PGE1, ONO-1608, U-10136, Prostin VR, Prostin Vr Pediatric, NSC-165559, Viridal 20, Prostaglandin E1, Caverject, Edex, Prostin, Viridal 5, Vitaros, Caverject Impulse, Alprostadil, Viridal 10, Viridal Duo)
  • EP1 receptor in Human [GtoPdb: 340] [UniProtKB: P34995]
  • EP1 receptor/Prostanoid EP1 receptor in Mouse [ChEMBL: CHEMBL2181] [GtoPdb: 340] [UniProtKB: P35375]
  • EP1 receptor in Rat [GtoPdb: 340] [UniProtKB: P70597]
1 CHEMBL495_lig_chart_1 EP1 receptor HumanMouseRat
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  • EP2 receptor in Human [GtoPdb: 341] [UniProtKB: P43116]
  • EP2 receptor/Prostanoid EP2 receptor in Mouse [ChEMBL: CHEMBL2488] [GtoPdb: 341] [UniProtKB: Q62053]
  • EP2 receptor in Rat [GtoPdb: 341] [UniProtKB: Q62928]
2 CHEMBL495_lig_chart_2 EP2 receptor HumanMouseRat
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  • EP3 receptor/Prostanoid EP3 receptor in Mouse [ChEMBL: CHEMBL4336] [GtoPdb: 342] [UniProtKB: P30557]
  • EP3 receptor in Rat [GtoPdb: 342] [UniProtKB: P34980]
3 CHEMBL495_lig_chart_3 Prostanoid EP3 receptor MouseRat
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  • EP4 receptor in Human [GtoPdb: 343] [UniProtKB: P35408]
  • EP4 receptor/Prostanoid EP4 receptor in Mouse [ChEMBL: CHEMBL2489] [GtoPdb: 343] [UniProtKB: P32240]
  • EP4 receptor in Rat [GtoPdb: 343] [UniProtKB: P43114]
4 CHEMBL495_lig_chart_4 EP4 receptor HumanMouseRat
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  • IP receptor/Prostanoid IP receptor in Human [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119]
  • IP receptor in Mouse [GtoPdb: 345] [UniProtKB: P43252]
5 CHEMBL495_lig_chart_5 Prostanoid IP receptor HumanMouse
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  • OATP2B1/Solute carrier organic anion transporter family member 2B1 in Rat [ChEMBL: CHEMBL2073698] [GtoPdb: 1224] [UniProtKB: Q9JHI3]
  • This target only has 0 pki data point
6 CHEMBL495_lig_chart_6 Solute carrier organic anion transporter family member 2B1 Rat
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  • DP1 receptor in Human [GtoPdb: 338] [UniProtKB: Q13258]
  • This target only has 1 pki data point
7 CHEMBL495_lig_chart_7 DP1 receptor Human
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  • CatSper1 in Human [GtoPdb: 388] [UniProtKB: Q8NEC5]
  • This target only has 0 pki data point
8 CHEMBL495_lig_chart_8 CatSper1 Human
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  • CatSper2 in Human [GtoPdb: 389] [UniProtKB: Q96P56]
  • This target only has 0 pki data point
9 CHEMBL495_lig_chart_9 CatSper2 Human
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  • CatSper3 in Human [GtoPdb: 390] [UniProtKB: Q86XQ3]
  • This target only has 0 pki data point
10 CHEMBL495_lig_chart_10 CatSper3 Human
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  • CatSper4 in Human [GtoPdb: 391] [UniProtKB: Q7RTX7]
  • This target only has 0 pki data point
11 CHEMBL495_lig_chart_11 CatSper4 Human
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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 27:

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]