Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T68782 Target Info
Target Name Prostaglandin D2 receptor (PTGDR)
Synonyms
Prostanoid DP receptor; PGD2 receptor; PGD receptor
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Target Type Clinical trial Target
Gene Name PTGDR
Biochemical Class GPCR rhodopsin
UniProt ID
PD2R_HUMAN
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 [3]
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 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) AMG 853 Drug Info IC50 = 3 nM Click to Show More [4]
2 Setipiprant Drug Info IC50 = 6 nM [5]
3 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 [1]
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 [1]
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 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 Discovery of AMG 853, a CRTH2 and DP Dual Antagonist. ACS Med Chem Lett. 2011 Mar 2;2(5):326-30.
REF 5 Identification of 2-(2-(1-naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic acid (setipiprant/ACT-129968), a potent, selective, and orally bioavailable chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2) antagonist. J Med Chem. 2013 Jun 27;56(12):4899-911.

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