Table 2SAR of 15-HPGD Inhibition

Image ml149fu11.jpg
AnalogueCIDSIDR1R2R3IC50 (μM)a
1324376099343745piperidine3-Me-PhH0.056
2299976337168053-Me-piperidineHH1.99
332394073239407morpholine4-OMe-PhMe2.23
432387924244157(CH2)2OMe3,4-F-PhH2.5
532442934250491(CH2)2OMe3-F-PhMe7.10
6324184742476711,4-dioxa-8-azaspiro[4.5]decane3-F-PhMe2.8
7324510342514121,4-dioxa-8-azaspiro[4.5]decanecyclohexylH7.9
832412624246991furfurylamine4-OMe-PhMe8.9
932455364251909furfurylamine2-OMe-PhH12.5
a

Note: all IC50 values represent the average of three experiments (n = 3). When tested in collaborator’s assay, an IC50 of 7.6nM was determined for the probe compound.

Note: all IC50 values represent the average of three experiments (n = 3). When tested in collaborator’s assay, an IC50 of 7.6nM was determined for the probe compound.

From: Potent and selective inhibitors of NAD+-dependent 15-hydroxyprostaglandin dehydrogenase (HPGD)

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Probe Reports from the NIH Molecular Libraries Program [Internet].

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