Literature summary for 3.4.16.2 extracted from

Graham, T.H.; Shu, M.; Verras, A.; Chen, Q.; Garcia-Calvo, M.; Li, X.; Lisnock, J.; Tong, X.; Tung, E.C.; Wiltsie, J.; Hale, J.J.; Pinto, S.; Shen, D.M.
Pyrazoles as non-classical bioisosteres in prolylcarboxypeptidase (PrCP) inhibitors (2014), Bioorg. Med. Chem. Lett., 24, 1657-1660.

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Inhibitors

Inhibitors	Comment	Organism	Structure
(3R,4R)-4-[3-(4-chlorophenyl)-1H-pyrazol-5-yl]-1-(2,2-dimethylpropyl)-3-(4-fluorophenyl)piperidine	compound shows improved oral bioavailabilities	Homo sapiens
(3R,4R)-4-[3-(4-chlorophenyl)-1H-pyrazol-5-yl]-1-(2,2-dimethylpropyl)-3-(4-fluorophenyl)piperidine	compound shows improved oral bioavailabilities	Mus musculus
2-[4-[3-(4-fluorophenyl)-1-methyl-1H-pyrazol-5-yl]-1-(2-phenylethyl)piperidin-4-yl]pyridine	most potent compound in the series	Homo sapiens
2-[4-[3-(4-fluorophenyl)-1-methyl-1H-pyrazol-5-yl]-1-(2-phenylethyl)piperidin-4-yl]pyridine	most potent compound in the series	Mus musculus

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-
Mus musculus	-	-	-

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.0000007	-	pH not specified in the publication, temperature not specified in the publication	Mus musculus	2-[4-[3-(4-fluorophenyl)-1-methyl-1H-pyrazol-5-yl]-1-(2-phenylethyl)piperidin-4-yl]pyridine
0.0000033	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	2-[4-[3-(4-fluorophenyl)-1-methyl-1H-pyrazol-5-yl]-1-(2-phenylethyl)piperidin-4-yl]pyridine
0.000066	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	(3R,4R)-4-[3-(4-chlorophenyl)-1H-pyrazol-5-yl]-1-(2,2-dimethylpropyl)-3-(4-fluorophenyl)piperidine
0.00018	-	pH not specified in the publication, temperature not specified in the publication	Mus musculus	(3R,4R)-4-[3-(4-chlorophenyl)-1H-pyrazol-5-yl]-1-(2,2-dimethylpropyl)-3-(4-fluorophenyl)piperidine

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Release 2023.1 (January 2023)