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Synonyms
carboxypeptidase, plasma carboxypeptidase, prolyl carboxypeptidase, lysosomal carboxypeptidase, carboxypeptidase a6, angiotensinase c, lysosomal pro-x carboxypeptidase, serine protease prolylcarboxypeptidase, matrix pk activator, proline carboxypeptidase,
more
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(3R,4R)-4-[3-(4-chlorophenyl)-1H-pyrazol-5-yl]-1-(2,2-dimethylpropyl)-3-(4-fluorophenyl)piperidine
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compound shows improved oral bioavailabilities
2-[4-[3-(4-fluorophenyl)-1-methyl-1H-pyrazol-5-yl]-1-(2-phenylethyl)piperidin-4-yl]pyridine
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most potent compound in the series
N-benzyloxycarbonyl-prolyl-prolinal
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the inhibition of PRCP activity by small molecule protease inhibitors administered peripherally or centrally decreased food intake in both wild-type and obese mice
potato carboxypeptidase inhibitor
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-
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t-butyl carbamate-prolyl-prolinal
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the inhibition of PRCP activity by small molecule protease inhibitors administered peripherally or centrally decreased food intake in both wild-type and obese mice
[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl](4-[(1Z)-1-[(2,5-dichlorophenyl)amino]-3-iminobut-1-en-1-yl]piperidin-1-yl)methanone
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compound has good levels of unbound compound in pure plasma
[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl](4-[(1Z)-1-[(3-chloro-4-fluorophenyl)amino]-3-iminoprop-1-en-1-yl]piperidin-1-yl)methanone
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compound achieves greater than 99% plasma target engagement with low brain exposure and has good levels of unbound compound in pure plasma
[4-[1-(3-chloro-4-fluorophenyl)-1H-pyrazol-5-yl]piperidin-1-yl][(1R,2R,4S)-2-(2,4-difluorophenyl)-4-(dimethylamino)-4-methylcyclopentyl]methanone
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compound has a superior in vivo profile, and also maintains a low brain to plasma ratio
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0.0000004 - 0.0000009
[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl](4-[(1Z)-1-[(2,5-dichlorophenyl)amino]-3-iminobut-1-en-1-yl]piperidin-1-yl)methanone
0.0000005 - 0.0000014
[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl](4-[(1Z)-1-[(3-chloro-4-fluorophenyl)amino]-3-iminoprop-1-en-1-yl]piperidin-1-yl)methanone
0.0000003 - 0.0000013
[4-[1-(3-chloro-4-fluorophenyl)-1H-pyrazol-5-yl]piperidin-1-yl][(1R,2R,4S)-2-(2,4-difluorophenyl)-4-(dimethylamino)-4-methylcyclopentyl]methanone
0.0000004
[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl](4-[(1Z)-1-[(2,5-dichlorophenyl)amino]-3-iminobut-1-en-1-yl]piperidin-1-yl)methanone
-
pH not specified in the publication, temperature not specified in the publication
0.0000009
[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl](4-[(1Z)-1-[(2,5-dichlorophenyl)amino]-3-iminobut-1-en-1-yl]piperidin-1-yl)methanone
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in 100% mouse plasma, pH not specified in the publication, temperature not specified in the publication
0.0000005
[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl](4-[(1Z)-1-[(3-chloro-4-fluorophenyl)amino]-3-iminoprop-1-en-1-yl]piperidin-1-yl)methanone
-
pH not specified in the publication, temperature not specified in the publication
0.0000014
[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl](4-[(1Z)-1-[(3-chloro-4-fluorophenyl)amino]-3-iminoprop-1-en-1-yl]piperidin-1-yl)methanone
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in 100% mouse plasma, pH not specified in the publication, temperature not specified in the publication
0.0000003
[4-[1-(3-chloro-4-fluorophenyl)-1H-pyrazol-5-yl]piperidin-1-yl][(1R,2R,4S)-2-(2,4-difluorophenyl)-4-(dimethylamino)-4-methylcyclopentyl]methanone
-
pH not specified in the publication, temperature not specified in the publication
0.0000013
[4-[1-(3-chloro-4-fluorophenyl)-1H-pyrazol-5-yl]piperidin-1-yl][(1R,2R,4S)-2-(2,4-difluorophenyl)-4-(dimethylamino)-4-methylcyclopentyl]methanone
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in 100% mouse plasma, pH not specified in the publication, temperature not specified in the publication
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0.00018
(3R,4R)-4-[3-(4-chlorophenyl)-1H-pyrazol-5-yl]-1-(2,2-dimethylpropyl)-3-(4-fluorophenyl)piperidine
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.0000007
2-[4-[3-(4-fluorophenyl)-1-methyl-1H-pyrazol-5-yl]-1-(2-phenylethyl)piperidin-4-yl]pyridine
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.0000004
[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl](4-[(1Z)-1-[(2,5-dichlorophenyl)amino]-3-iminobut-1-en-1-yl]piperidin-1-yl)methanone
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.0000003
[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl](4-[(1Z)-1-[(3-chloro-4-fluorophenyl)amino]-3-iminoprop-1-en-1-yl]piperidin-1-yl)methanone
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.0000002
[4-[1-(3-chloro-4-fluorophenyl)-1H-pyrazol-5-yl]piperidin-1-yl][(1R,2R,4S)-2-(2,4-difluorophenyl)-4-(dimethylamino)-4-methylcyclopentyl]methanone
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
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Wang, X.; Smith, P.L.; Hsu, M.Y.; Tamasi, J.A.; Bird, E.; Schumacher, W.A.
Deficiency in thrombin-activatable fibrinolysis inhibitor (TAFI) protected mice from ferric chloride-induced vena cava thrombosis
J. Thromb. Thrombolysis
23
41-49
2007
Mus musculus
brenda
Palmiter, R.D.
Reduced levels of neurotransmitter-degrading enzyme PRCP promote obesity
J. Clin. Invest.
119
2130-2133
2009
Mus musculus (Q7TMR0)
brenda
Wallingford, N.; Perroud, B.; Gao, Q.; Coppola, A.; Gyengesi, E.; Liu, Z.W.; Gao, X.B.; Diament, A.; Haus, K.A.; Shariat-Madar, Z.; Mahdi, F.; Wardlaw, S.L.; Schmaier, A.H.; Warden, C.H.; Diano, S.
Prolylcarboxypeptidase regulates food intake by inactivating alpha-MSH in rodents
J. Clin. Invest.
119
2291-2303
2009
Mus musculus
brenda
Graham, T.H.; Liu, W.; Verras, A.; Sebhat, I.K.; Xiong, Y.; Bleasby, K.; Bhatt, U.R.; Chen, Q.; Garcia-Calvo, M.; Geissler, W.M.; Gorski, J.N.; He, H.; Lassman, M.E.; Lisnock, J.; Li, X.; Shen, Z.; Tong, X.; Tung, E.C.; Wiltsie, J.; Xiao, J.; Xie, D.; Xu, S.; Hale, J.J.; Pinto, S.; Shen, D.M.
A new class of prolylcarboxypeptidase inhibitors, part 1: discovery and evaluation
Bioorg. Med. Chem. Lett.
22
2811-2817
2012
Homo sapiens, Mus musculus
brenda
Graham, T.H.; Liu, W.; Verras, A.; Reibarkh, M.; Bleasby, K.; Bhatt, U.R.; Chen, Q.; Garcia-Calvo, M.; Geissler, W.M.; Gorski, J.N.; He, H.; Lassman, M.E.; Lisnock, J.; Li, X.; Shen, Z.; Tong, X.; Tung, E.C.; Wiltsie, J.; Xie, D.; Xu, S.; Xiao, J.; Hale, J.J.; Pinto, S.; Shen, D.M.
A new class of prolylcarboxypeptidase inhibitors, part 2: the aminocyclopentanes
Bioorg. Med. Chem. Lett.
22
2818-2822
2012
Homo sapiens, Mus musculus
brenda
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
Bioorg. Med. Chem. Lett.
24
1657-1660
2014
Homo sapiens, Mus musculus
brenda
Jeong, J.K.; Diano, S.
Prolyl carboxypeptidase mRNA expression in the mouse brain
Brain Res.
1542
85-92
2014
Mus musculus
brenda
Grobe, N.; Weir, N.M.; Leiva, O.; Ong, F.S.; Bernstein, K.E.; Schmaier, A.H.; Morris, M.; Elased, K.M.
Identification of prolyl carboxypeptidase as an alternative enzyme for processing of renal angiotensin II using mass spectrometry
Am. J. Physiol. Cell Physiol.
304
C945-C953
2013
Mus musculus
brenda