Target Validation Information
Target ID T87023
Target Name Platelet-activating factor receptor
Target Type
Successful
Drug Potency against Target MK-287 Drug Info IC50 = 6 nM [534630]
RUPATADINE Drug Info IC50 = 3700 nM [527799]
SDZ-64-412 Drug Info IC50 = 60 nM [533935]
L-659989 Drug Info Ki = 9 nM [526814]
VERAGUENSIN Drug Info Ki = 1000 nM [526814]
L-652731 Drug Info Ki = 103 nM [526814]
SCH-37370 Drug Info IC50 = 840 nM [527799]
Apafant Drug Info IC50 = 17 nM [552872]
References
Ref 534630J Med Chem. 1998 May 21;41(11):1970-9.(+/-)-trans-2-[3-methoxy-4-(4-chlorophenylthioethoxy)-5-(N-methyl-N- hydroxyureidyl)methylphenyl]-5-(3,4, 5-trimethoxyphenyl)tetrahydrofuran (CMI-392), a potent dual 5-lipoxygenase inhibitor and platelet-activating factor receptor antagonist.
Ref 527799J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm.
Ref 533935J Med Chem. 1993 Oct 15;36(21):3098-102.Structural modification of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinoline platelet activating factor receptor antagonists.
Ref 526814J Med Chem. 1992 Sep 18;35(19):3474-82.Development, synthesis, and biological evaluation of (-)-trans-(2S,5S)-2-[3-[(2-oxopropyl)sulfonyl]-4-n-propoxy-5-(3- hydroxypropoxy)-phenyl]-5-(3,4,5-trimethoxyphenyl)tetrahydrofuran, a potent orally active platelet-activating factor (PAF) antagonist and its water-soluble prodrug phosphate ester.
Ref 526814J Med Chem. 1992 Sep 18;35(19):3474-82.Development, synthesis, and biological evaluation of (-)-trans-(2S,5S)-2-[3-[(2-oxopropyl)sulfonyl]-4-n-propoxy-5-(3- hydroxypropoxy)-phenyl]-5-(3,4,5-trimethoxyphenyl)tetrahydrofuran, a potent orally active platelet-activating factor (PAF) antagonist and its water-soluble prodrug phosphate ester.
Ref 526814J Med Chem. 1992 Sep 18;35(19):3474-82.Development, synthesis, and biological evaluation of (-)-trans-(2S,5S)-2-[3-[(2-oxopropyl)sulfonyl]-4-n-propoxy-5-(3- hydroxypropoxy)-phenyl]-5-(3,4,5-trimethoxyphenyl)tetrahydrofuran, a potent orally active platelet-activating factor (PAF) antagonist and its water-soluble prodrug phosphate ester.
Ref 527799J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm.
Ref 552872The 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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