Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T76198 | Target Info | |||
| Target Name | Thromboxane A2 receptor (TBXA2R) | ||||
| Synonyms |
TXA2-R; TXA2 receptor; Prostanoid TP receptor
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| Target Type | Successful Target | ||||
| Gene Name | TBXA2R | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| 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 | [1] | ||
| 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 | [2] | ||
| 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 | [3] | ||
| 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 | [3] | ||
| Co-Target Name | Thromboxane-A synthase (TBXAS1) | Clinical trial Target | ||||
| UniProt ID | THAS_HUMAN | |||||
| Gene Name | TBXAS1 | |||||
| Synonyms |
Thromboxane A2 synthase; TXS; TXA synthase; Cytochrome P450 5A1; CYP5A1; CYP5
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| Representative Drug(s) | Ridogrel | Drug Info | IC50 = 3 nM | Click to Show More | [4] | |
| 2 | BIBV 308 | Drug Info | IC50 = 4 nM | [5] | ||
| 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) | Ramatroban | Drug Info | Ki = 4.3 nM | Click to Show More | [6] | |
| 2 | LAROPIPRANT | Drug Info | Ki = 745 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) | PGF2alpha | Drug Info | IC50 = 110 nM | Click to Show More | [7] | |
| 2 | LAROPIPRANT | Drug Info | Ki = 892 nM | [3] | ||
| 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) | PGF2alpha | Drug Info | IC50 = 220 nM | [7] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Design and synthesis of a highly selective EP2-receptor agonist. Bioorg Med Chem Lett. 2001 Aug 6;11(15):2025-8. | ||||
| REF 2 | Synthesis and in vitro evaluation of human FP-receptor selective prostaglandin analogues. Bioorg Med Chem Lett. 2000 Jul 17;10(14):1519-22. | ||||
| REF 3 | 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 4 | Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-(3-(3-pyridinyl) propyl)octanoic acid and analogs. J Med Chem. 1992 Nov 13;35(23):4373-83. | ||||
| REF 5 | Guanidine derivatives as combined thromboxane A2 receptor antagonists and synthase inhibitors. J Med Chem. 1999 Apr 8;42(7):1235-49. | ||||
| REF 6 | Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist. J Med Chem. 2005 Feb 24;48(4):897-900. | ||||
| REF 7 | 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. | ||||
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