Protein Information

General Information of the Protein

Protein ID	PT01037
Protein Name	Prolyl endopeptidase
Secondarily Protein Name	Post-proline cleaving enzyme
Gene Name	PREP
Secondarily Gene Name	PEP
Sequence	MLSLQYPDVYRDETAVQDYHGHKICDPYAWLEDPDSEQTKAFVEAQNKITVPFLEQCPIRGLYKERMTELYDYPKYSCHFKKGKRYFYFYNTGLQNQRVLYVQDSLEGEARVFLDPNILSDDGTVALRGYAFSEDGEYFAYGLSASGSDWVTIKFMKVDGAKELPDVLERVKFSCMAWTHDGKGMFYNSYPQQDGKSDGTETSTNLHQKLYYHVLGTDQSEDILCAEFPDEPKWMGGAELSDDGRYVLLSIREGCDPVNRLWYCDLQQESSGIAGILKWVKLIDNFEGEYDYVTNEGTVFTFKTNRQSPNYRVINIDFRDPEESKWKVLVPEHEKDVLEWIACVRSNFLVLCYLHDVKNILQLHDLTTGALLKTFPLDVGSIVGYSGQKKDTEIFYQFTSFLSPGIIYHCDLTKEELEPRVFREVTVKGIDASDYQTVQIFYPSKDGTKIPMFIVHKKGIKLDGSHPAFLYGYGGFNISITPNYSVSRLIFVRHMGGILAVANIRGGGEYGETWHKGGILANKQNCFDDFQCAAEYLIKEGYTSPKRLTINGGSNGGLLVAACANQRPDLFGCVIAQVGVMDMLKFHKYTIGHAWTTDYGCSDSKQHFEWLVKYSPLHNVKLPEADDIQYPSMLLLTADHDDRVVPLHSLKFIATLQYIVGRSRKQSNPLLIHVDTKAGHGAGKPTAKVIEEVSDMFAFIARCLNVDWIP Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Enzyme > Protease > Serine protease > Serine protease SC clan > Serine protease S9A subfamily
Function	Cleaves peptide bonds on the C-terminal side of prolyl residues within peptides that are up to approximately 30 amino acids long. Show/Hide
Uniprot ID	Primary ID: P48147 Secondarily ID: Q8N6D4 Show/Hide
Ensembl ID	ENSG00000085377
HGNC ID	HGNC:9358
Subcellular Location	Cytoplasm

Map of Molecular Bioactivity Related to the Protein

Map of Molecular Bioactivity Related to the Protein Protein Cell Line Compound Bioactivity Value: <= 0.1 μM > 0.1 μM and <= 10 μM > 10 μM Imprecise Activity

Table of Molecular Bioactivities Related to the Protein

Cell Line ID: CL000419 , HCE-T

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0044004 Compound Info	benzyl N-[(2S)-1-[(2S)-2-cyanopyrrolidin-1-yl]-1-oxopropan-2-yl]carbamate Show/Hide	C16H19N3O3	1
1	IC50 = 20 nM Bioactivity Info	TI LI LO TS
CP0075193 Compound Info	benzyl N-[2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]carbamate Show/Hide	C15H17N3O3	1
1	IC50 = 180 nM Bioactivity Info	TI LI LO TS
CP0043934 Compound Info	(2R,5S,7R)-1-Aza-7-benzyloxycarbonylamino-8-oxo-4-thiabicyclo[3.3.0]octane-2-carbonitrile Show/Hide	C15H15N3O3S	1
1	IC50 = 1300 nM Bioactivity Info	TI LI LO TS
CP0166361 Compound Info	benzyl N-[2-[(2R)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]carbamate Show/Hide	C15H17N3O3	1
1	IC50 = 2800 nM Bioactivity Info	TI LI LO TS
CP0181871 Compound Info	benzyl N-[(2R)-1-[(2S)-2-cyanopyrrolidin-1-yl]-1-oxopropan-2-yl]carbamate Show/Hide	C16H19N3O3	1
1	IC50 = 6600 nM Bioactivity Info	TI LI LO TS

Cell Line Info

Cell Line Info

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0044004 Compound Info	benzyl N-[(2S)-1-[(2S)-2-cyanopyrrolidin-1-yl]-1-oxopropan-2-yl]carbamate Show/Hide	C16H19N3O3	2
1	IC50 = 3 nM
2	IC50 = 5 nM
CP0075193 Compound Info	benzyl N-[2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]carbamate Show/Hide	C15H17N3O3	1
1	IC50 = 20 nM
CP0046436 Compound Info	(2S)-1-(2-benzyl-3-oxo-1H-isoindole-4-carbonyl)pyrrolidine-2-carbonitrile Show/Hide	C21H19N3O2	4
1	IC50 = 45 nM
2	IC50 < 50 nM
3	IC50 = 81 nM
4	Ki = 25 nM
CP0086237 Compound Info	N-benzyl-2-[(2S)-2-cyanopyrrolidine-1-carbonyl]benzamide Show/Hide	C20H19N3O2	4
1	IC50 < 50 nM
2	IC50 = 65 nM
3	IC50 = 68 nM
4	IC50 = 73 nM
CP0046339 Compound Info	2-benzyl-7-(pyrrolidine-1-carbonyl)-3H-isoindol-1-one Show/Hide	C20H20N2O2	5
1	IC50 = 150 nM
2	IC50 = 350 nM
3	IC50 = 500 nM
4	IC50 = 620 nM
5	Ki = 160 nM
CP0043934 Compound Info	(2R,5S,7R)-1-Aza-7-benzyloxycarbonylamino-8-oxo-4-thiabicyclo[3.3.0]octane-2-carbonitrile Show/Hide	C15H15N3O3S	2
1	IC50 = 200 nM
2	IC50 = 500 nM
CP0166361 Compound Info	benzyl N-[2-[(2R)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]carbamate Show/Hide	C15H17N3O3	1
1	IC50 = 430 nM
CP0181871 Compound Info	benzyl N-[(2R)-1-[(2S)-2-cyanopyrrolidin-1-yl]-1-oxopropan-2-yl]carbamate Show/Hide	C16H19N3O3	2
1	IC50 = 1200 nM
2	IC50 = 1400 nM

Clinical Information about the Protein

Target 1 ( Prolyl endopeptidase (PREP) )

Target Type	Clinical trial Target
Disease	4 Target-related Diseases				4
1	Influenza virus infection [ICD-11: 1E30-1E32]
2	Cognitive impairment [ICD-11: 6D71]
3	Parkinson disease [ICD-11: 8A00.0]
4	Human immunodeficiency virus infection [ICD-11: 1C62]
Clinical Trial Drug(s)	3 Clinical Trial Drugs				3
1	BAICALEIN	Drug Info	Phase 2	Influenza virus infection
2	ONO-1603	Drug Info	Phase 2	Cognitive impairment
3	S-17092-1	Drug Info	Phase 1	Cognitive impairment
Discontinued Drug(s)	3 Discontinued Drugs				3
1	JTP-4819	Drug Info	Discontinued in Phase 2	Cognitive impairment
2	Z-321	Drug Info	Discontinued in Phase 1	Parkinson disease
3	BAICALIN	Drug Info	Terminated	Human immunodeficiency virus infection