Target Validation Information
Target ID T59626
Target Name Leukotriene B4 receptor 1
Target Type
Discontinued
Drug Potency against Target SC-41390 Drug Info IC50 = 1 nM
SC-50073 Drug Info IC50 = 0.85 nM
(3S,4R)-3-Benzyl-7-isopropyl-chroman-4-ol Drug Info IC50 = 7200 nM
SC-51146 Drug Info IC50 = 10.9 nM
DTPA Conjugate Drug Info IC50 = 30 nM [527773]
HYNIC Analogue Drug Info IC50 = 44 nM [527773]
CP-105696 Drug Info IC50 = 5 nM
SB-201993 Drug Info Ki = 7.1 nM [534210]
LY293111 Drug Info IC50 = 17 nM
LEUKOTRIENE_B4 Drug Info IC50 = 32 nM
SC-50135 Drug Info IC50 < 0.1 nM
SC-53229 Drug Info IC50 = 8.5 nM
LEUCETTAMIDINE Drug Info Ki = 5300 nM
SC-52569 Drug Info IC50 = 0.15 nM
SC-52073 Drug Info IC50 = 0.1 nM
SC-50676 Drug Info IC50 = 5.3 nM
LEUCETTAMINE A Drug Info IC50 = 4600 nM
SB-201146 Drug Info Ki = 4.7 nM [534210]
LY-282210 Drug Info IC50 = 47 nM [533960]
LY-292728 Drug Info IC50 = 1.2 nM [533960]
(LTB4-(Csa)4)2-Glu-H Conjugate Drug Info IC50 = 8 nM [527773]
SC-53228 Drug Info IC50 = 14.5 nM
The Effect of Target Knockout, Knockdown or Genetic Variations Decreased extravasation in intraperitoneal zymosan challenge; 5-lipoxygenase KOs have decreased airway responsiveness in the ovalb uMin challenge and reduced pulmonary fibrosis.
References
Ref 527773J Med Chem. 2005 Oct 6;48(20):6442-53.Synthesis of leukotriene B4 antagonists labeled with In-111 or Tc-99m to image infectious and inflammatory foci.
Ref 527773J Med Chem. 2005 Oct 6;48(20):6442-53.Synthesis of leukotriene B4 antagonists labeled with In-111 or Tc-99m to image infectious and inflammatory foci.
Ref 534210J Med Chem. 1996 Sep 13;39(19):3837-41.(E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid: a high-affinity leukotriene B4 receptor antagonist with oral antiinflammatory activity.
Ref 534210J Med Chem. 1996 Sep 13;39(19):3837-41.(E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid: a high-affinity leukotriene B4 receptor antagonist with oral antiinflammatory activity.
Ref 533960J Med Chem. 1993 Nov 26;36(24):3982-4.Biphenylyl-substituted xanthones: highly potent leukotriene B4 receptor antagonists.
Ref 533960J Med Chem. 1993 Nov 26;36(24):3982-4.Biphenylyl-substituted xanthones: highly potent leukotriene B4 receptor antagonists.
Ref 527773J Med Chem. 2005 Oct 6;48(20):6442-53.Synthesis of leukotriene B4 antagonists labeled with In-111 or Tc-99m to image infectious and inflammatory foci.

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