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 534630 | J 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 527799 | J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm. | ||||
Ref 533935 | J 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 526814 | J 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 526814 | J 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 526814 | J 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 527799 | J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm. | ||||
Ref 552872 | 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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