Target Validation Information
TTD ID T87023
Target Name Platelet-activating factor receptor (PTAFR)
Type of Target
Successful
Drug Potency against Target DE-081 Drug Info IC50 = 17 nM [5]
L-652731 Drug Info Ki = 103 nM [1]
L-659989 Drug Info Ki = 9 nM [1]
MK-287 Drug Info IC50 = 6 nM [4]
PegCNTF Drug Info IC50 = 840 nM [2]
RUPATADINE Drug Info IC50 = 3700 nM [2]
SDZ-64-412 Drug Info IC50 = 60 nM [3]
VERAGUENSIN Drug Info Ki = 1000 nM [1]
References
REF 1 Development, synthesis, and biological evaluation of (-)-trans-(2S,5S)-2-[3-[(2-oxopropyl)sulfonyl]-4-n-propoxy-5-(3- hydroxypropoxy)-phenyl]-5-(3,... J Med Chem. 1992 Sep 18;35(19):3474-82.
REF 2 Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.
REF 3 Structural modification of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinoline platelet activating factor receptor antagonists. J Med Chem. 1993 Oct 15;36(21):3098-102.
REF 4 (+/-)-trans-2-[3-methoxy-4-(4-chlorophenylthioethoxy)-5-(N-methyl-N- hydroxyureidyl)methylphenyl]-5-(3,4, 5-trimethoxyphenyl)tetrahydrofuran (CMI-3... J Med Chem. 1998 May 21;41(11):1970-9.
REF 5 The exploding field of the HCV polymerase non-nucleoside inhibitors: summary of a first generation compounds. Mini Rev Med Chem. 2008 Oct;8(12):1298-310.

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