Table 2, SAR of 15-HPGD Inhibition - Probe Reports from the NIH Molecular Libraries Program - NCBI Bookshelf

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Table 2SAR of 15-HPGD Inhibition


Analogue	CID	SID	R₁	R₂	R₃	IC50 (μM)^a
1	3243760	99343745	piperidine	3-Me-Ph	H	0.056
2	2999763	3716805	3-Me-piperidine	H	H	1.99
3	3239407	3239407	morpholine	4-OMe-Ph	Me	2.23
4	3238792	4244157	(CH₂)₂OMe	3,4-F-Ph	H	2.5
5	3244293	4250491	(CH₂)₂OMe	3-F-Ph	Me	7.10
6	3241847	4247671	1,4-dioxa-8-azaspiro[4.5]decane	3-F-Ph	Me	2.8
7	3245103	4251412	1,4-dioxa-8-azaspiro[4.5]decane	cyclohexyl	H	7.9
8	3241262	4246991	furfurylamine	4-OMe-Ph	Me	8.9
9	3245536	4251909	furfurylamine	2-OMe-Ph	H	12.5

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.

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

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