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Drug-Target Interaction

Drug

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PubChem ID:173727
Structure:
Synonyms:
1-(4-(3-(4-(Bis(4-fluorophenyl)hydroxymethyl)-1-piperidinyl)propoxy)-3-met
1-(4-(3-(4-(Bis(4-fluorophenyl)hydroxymethyl)-1-piperidinyl)propoxy)-3-methoxyphenyl)ethanone
60284-71-1
AC1L5AFB
Ahr 5333
Ahr-5333
CHEBI:119336
CHEMBL17436
CID173727
Ethanone, 1-(4-(3-(4-(bis(4-fluorophenyl)hydroxymethyl)-1-piperidinyl)propoxy)-3-methoxyphenyl)-

Target

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Uniprot ID:Q6LCE7_HUMAN
Synonyms:
Cyclooxygenase-1
EC-Numbers:1.14.99.1
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

2554366
1-[4-[3-[4-[bis(4-fluorophenyl)hydroxymethyl]-1- piperidinyl]propoxy]-3-methoxyphenyl]ethanone(AHR-5333): a selective human blood neutrophil 5-lipoxygenase inhibitor.. G Graff; L A Anderson (1989) Prostaglandins display abstract
In this study we report the in vitro inhibition of leukotriene synthesis in calcium ionophore (A23187)-stimulated, intact human blood neutrophils by AHR-5333. The results showed that AHR-5333 inhibits 5-HETE, LTB4 and LTC4 synthesis with IC50 values of 13.9, 13.7 and 6.9 microM, respectively. Further examination of the effect of AHR-5333 on individual reactions of the 5-lipoxygenase pathway (i.e. conversion of LTA4 to LTB4, LTA4 to LTC4, and arachidonic acid to 5-HETE) showed that this agent was not inhibitory to LTA4 epoxyhydrolase and glutathione-S-transferase activity in neutrophil homogenates. However, conversion of arachidonic acid (30 microM) to 5-HETE was half maximally inhibited by 20 microM AHR-5333 in the cell-free system. The inhibition of LTB4 and LTC4 formation in intact neutrophils by AHR-5333 appears to be entirely due to a selective inhibition of 5-lipoxygenase activity and an impaired formation of LTA4, which serves as substrate for LTA4 epoxyhydrolase and glutathione-S-transferase. AHR-5333 did not affect the transformation of exogenous arachidonic acid to thromboxane B2, HHT and 12-HETE in preparations of washed human platelets, indicating that this agent has no effect on platelet prostaglandin H synthase, thromboxane synthase and 12-lipoxygenase activity. The lack of inhibitory activity of AHR-5333 on prostaglandin H synthase activity was confirmed with microsomal preparations of sheep vesicular glands.