Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T38529 | Target Info | |||
| Target Name | Prostaglandin E2 receptor EP2 (PTGER2) | ||||
| Synonyms |
Prostanoid EP2 receptor; Prostaglandin E2 receptor EP2 subtype; PGE2 receptor EP2 subtype; PGE receptor, EP2 subtype; PGE receptor EP2 subtype; EP2 receptor
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| Target Type | Successful Target | ||||
| Gene Name | PTGER2 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Thromboxane A2 receptor (TBXA2R) | Successful Target | ||||
| UniProt ID | TA2R_HUMAN | |||||
| Gene Name | TBXA2R | |||||
| Synonyms |
TXA2-R; TXA2 receptor; Prostanoid TP receptor
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| Representative Drug(s) | PGF2alpha | Drug Info | IC50 ~ 0.001 nM | Click to Show More | [1] | |
| 2 | LAROPIPRANT | Drug Info | Ki = 2.95 nM | [5] | ||
| Co-Target Name | Prostacyclin receptor (PTGIR) | Successful Target | ||||
| UniProt ID | PI2R_HUMAN | |||||
| Gene Name | PTGIR | |||||
| Synonyms |
Prostanoid IP receptor; Prostaglandin I2 receptor; PRIPR; PGI2 receptor; PGI receptor; IP prostanoid receptor
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| Representative Drug(s) | Alprostadil | Drug Info | EC50 = 1.8 nM | Click to Show More | [2] | |
| 2 | Iloprost | Drug Info | EC50 = 2.4 nM | [3] | ||
| 3 | Dinoprostone | Drug Info | IC50 = 260 nM | [7] | ||
| Co-Target Name | Prostaglandin F2-alpha receptor (PTGFR) | Successful Target | ||||
| UniProt ID | PF2R_HUMAN | |||||
| Gene Name | PTGFR | |||||
| Synonyms |
Prostanoid FP receptor; PGF2-alpha receptor; PGF2 alpha receptor; PGF receptor; FP prostanoid receptor; FP prostaglandin receptor
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| Representative Drug(s) | PGF2alpha | Drug Info | IC50 = 2.5 nM | Click to Show More | [4] | |
| 2 | Dinoprostone | Drug Info | EC50 = 250 nM | [6] | ||
| Co-Target Name | Prostaglandin E2 receptor EP4 (PTGER4) | Clinical trial Target | ||||
| UniProt ID | PE2R4_HUMAN | |||||
| Gene Name | PTGER4 | |||||
| Synonyms |
Prostanoid EP4 receptor; Prostaglandin E2 receptor EP4 subtype; PTGER2; PGE2 receptor EP4 subtype; PGE receptor EP4 subtype
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| Representative Drug(s) | Dinoprostone | Drug Info | EC50 = 0.02 nM | [8] | ||
| Co-Target Name | Prostaglandin D2 receptor (PTGDR) | Clinical trial Target | ||||
| UniProt ID | PD2R_HUMAN | |||||
| Gene Name | PTGDR | |||||
| Synonyms |
Prostanoid DP receptor; PGD2 receptor; PGD receptor
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| Representative Drug(s) | LAROPIPRANT | Drug Info | IC50 = 0.09 nM | Click to Show More | [5] | |
| 2 | Iloprost | Drug Info | EC50 = 147 nM | [3] | ||
| Co-Target Name | Prostaglandin E2 receptor EP3 (PTGER3) | Clinical trial Target | ||||
| UniProt ID | PE2R3_HUMAN | |||||
| Gene Name | PTGER3 | |||||
| Synonyms |
Prostanoid EP3 receptor; Prostaglandin E2 receptor EP3 subtype; PGE2-R; PGE2 receptor EP3 subtype; PGE receptor, EP3 subtype; PGE receptor EP3 subtype
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| Representative Drug(s) | Dinoprostone | Drug Info | Ki = 0.33 nM | Click to Show More | [9] | |
| 2 | PGF2alpha | Drug Info | IC50 = 110 nM | [1] | ||
| 3 | LAROPIPRANT | Drug Info | Ki = 892 nM | [5] | ||
| Co-Target Name | Prostaglandin E2 receptor EP1 (PTGER1) | Clinical trial Target | ||||
| UniProt ID | PE2R1_HUMAN | |||||
| Gene Name | PTGER1 | |||||
| Synonyms |
Prostanoid EP1 receptor; Prostaglandin E2 receptor EP1 subtype; PGE2 receptor EP1 subtype; PGE receptor, EP1 subtype; PGE receptor EP1 subtype; EP1 receptor
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| Representative Drug(s) | Dinoprostone | Drug Info | IC50 = 1.1 nM | Click to Show More | [10] | |
| 2 | PGF2alpha | Drug Info | IC50 = 220 nM | [1] | ||
| Co-Target Name | Prostaglandin D2 receptor 2 (PTGDR2) | Clinical trial Target | ||||
| UniProt ID | PD2R2_HUMAN | |||||
| Gene Name | PTGDR2 | |||||
| Synonyms |
PTGDR2; Chemoattractant receptor-homologous molecule expressed on Th2 cells; CD294
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| Representative Drug(s) | LAROPIPRANT | Drug Info | Ki = 745 nM | [5] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Synthesis and biological evaluation of prostaglandin-F alkylphosphinic acid derivatives as bone anabolic agents for the treatment of osteoporosis. J Med Chem. 2001 Nov 22;44(24):4157-69. | ||||
| REF 2 | Design and synthesis of a highly selective EP2-receptor agonist. Bioorg Med Chem Lett. 2001 Aug 6;11(15):2025-8. | ||||
| REF 3 | Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension. J Med Chem. 2017 Feb 9;60(3):913-927. | ||||
| REF 4 | Synthesis and in vitro evaluation of human FP-receptor selective prostaglandin analogues. Bioorg Med Chem Lett. 2000 Jul 17;10(14):1519-22. | ||||
| REF 5 | Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydroc... J Med Chem. 2007 Feb 22;50(4):794-806. | ||||
| REF 6 | Discovery of G Protein-Biased EP2 Receptor Agonists. ACS Med Chem Lett. 2016 Jan 4;7(3):306-11. | ||||
| REF 7 | Prostanoid receptor EP2 as a therapeutic target. J Med Chem. 2014 Jun 12;57(11):4454-65. | ||||
| REF 8 | Difluoromethylene at the gamma-Lactam alpha-Position Improves 11-Deoxy-8-aza-PGE 1 Series EP 4 Receptor Binding and Activity: 11-Deoxy-10,10-difluoro-8-aza-PGE 1 Analog (KMN-159) as a Potent EP 4 Agonist. J Med Chem. 2019 May 9;62(9):4731-4741. | ||||
| REF 9 | Synthesis and evaluation of a gamma-lactam as a highly selective EP2 and EP4 receptor agonist. Bioorg Med Chem Lett. 2008 Jan 15;18(2):821-4. | ||||
| REF 10 | Emerging targets in osteoporosis disease modification. J Med Chem. 2010 Jun 10;53(11):4332-53. | ||||
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