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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