Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T99954 | Target Info | |||
| Target Name | Prostacyclin receptor (PTGIR) | ||||
| Synonyms |
Prostanoid IP receptor; Prostaglandin I2 receptor; PRIPR; PGI2 receptor; PGI receptor; IP prostanoid receptor
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| Target Type | Successful Target | ||||
| Gene Name | PTGIR | ||||
| 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) | LAROPIPRANT | Drug Info | Ki = 2.95 nM | [1] | ||
| Co-Target Name | Prostaglandin E2 receptor EP2 (PTGER2) | Successful Target | ||||
| UniProt ID | PE2R2_HUMAN | |||||
| Gene Name | 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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| Representative Drug(s) | LAROPIPRANT | Drug Info | Ki = 136 nM | Click to Show More | [1] | |
| 2 | Ralinepag | Drug Info | Ki = 610 nM | [2] | ||
| 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 | [1] | |
| 2 | Selexipag | Drug Info | EC50 = 100 nM | [2] | ||
| 3 | Ralinepag | Drug Info | EC50 = 850 nM | [2] | ||
| 4 | Ralinepag | Drug Info | EC50 = 980 nM | [2] | ||
| 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) | Ralinepag | Drug Info | Ki = 143 nM | Click to Show More | [2] | |
| 2 | LAROPIPRANT | Drug Info | Ki = 892 nM | [1] | ||
| 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) | Ralinepag | Drug Info | Ki = 678 nM | [2] | ||
| 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 | [1] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | 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 2 | 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. | ||||
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