General Information of the Protein
Protein ID
PT01428
Protein Name
Glutaminyl-peptide cyclotransferase
Secondarily
Protein Name
Glutaminyl cyclase
Glutaminyl-tRNA cyclotransferase
Glutamyl cyclase
Gene Name
QPCT
Sequence
MAGGRHRRVVGTLHLLLLVAALPWASRGVSPSASAWPEEKNYHQPAILNSSALRQIAEGTSISEMWQNDLQPLLIERYPGSPGSYAARQHIMQRIQRLQADWVLEIDTFLSQTPYGYRSFSNIISTLNPTAKRHLVLACHYDSKYFSHWNNRVFVGATDSAVPCAMMLELARALDKKLLSLKTVSDSKPDLSLQLIFFDGEEAFLHWSPQDSLYGSRHLAAKMASTPHPPGARGTSQLHGMDLLVLLDLIGAPNPTFPNFFPNSARWFERLQAIEHELHELGLLKDHSLEGRYFQNYSYGGVIQDDHIPFLRRGVPVLHLIPSPFPEVWHTMDDNEENLDESTIDNLNKILQVFVLEYLHL
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Aminoacyltransferase
Function
Responsible for the biosynthesis of pyroglutamyl peptides. Has a bias against acidic and tryptophan residues adjacent to the N-terminal glutaminyl residue and a lack of importance of chain length after the second residue. Also catalyzes N-terminal pyroglutamate formation. In vitro, catalyzes pyroglutamate formation of N-terminally truncated form of APP amyloid-beta peptides [Glu-3]-amyloid-beta. May be involved in the N-terminal pyroglutamate formation of several amyloid-related plaque-forming peptides.
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Uniprot ID
Primary ID:
Q16769

Secondarily ID:
Q16770
Q3KRG6
Q53TR4
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Ensembl ID
ENSG00000115828
HGNC ID
HGNC:9753
Subcellular Location
Secreted
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: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0446889
1-(2,3-dihydro-1,4-benzodioxin-6-yl)-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C16H20N4O2S
 1
1
IC50 = 58 nM
   TI
   LI
   LO
   TS
CP0370024
1-(3,4-Dimethoxyphenyl)-3-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea
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C16H22N4O2S
 1
1
IC50 = 119 nM
   TI
   LI
   LO
   TS
CP0508660
3-[3-(5-methylimidazol-1-yl)propyl]-1H-quinazoline-2,4-dione
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C15H16N4O2
 1
1
IC50 = 123 nM
   TI
   LI
   LO
   TS
CP0397489
1-isoquinolin-1-yl-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C17H19N5S
 1
1
IC50 = 158 nM
   TI
   LI
   LO
   TS
CP0435687
1-(1,3-benzodioxol-5-yl)-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C15H18N4O2S
 1
1
IC50 = 185 nM
   TI
   LI
   LO
   TS
CP0508663
1-(3,4-dihydro-2H-chromen-6-yl)-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C17H22N4OS
 1
1
IC50 = 208 nM
   TI
   LI
   LO
   TS
CP0540385
1-[3-(5-methylimidazol-1-yl)propyl]-3-(1-methylindazol-6-yl)thiourea
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C16H20N6S
 1
1
IC50 = 239 nM
   TI
   LI
   LO
   TS
CP0397331
1-[3-(5-methylimidazol-1-yl)propyl]-3-quinolin-6-ylthiourea
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C17H19N5S
 1
1
IC50 = 293 nM
   TI
   LI
   LO
   TS
CP0508658
1-(2-methyl-1,3-benzoxazol-6-yl)-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C16H19N5OS
 1
1
IC50 = 329 nM
   TI
   LI
   LO
   TS
CP0423024
1-[3-(5-methylimidazol-1-yl)propyl]-3-quinolin-2-ylthiourea
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C17H19N5S
 1
1
IC50 = 337 nM
   TI
   LI
   LO
   TS
CP0540383
1-[3-(5-methylimidazol-1-yl)propyl]-3-quinolin-5-ylthiourea
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C17H19N5S
 1
1
IC50 = 375 nM
   TI
   LI
   LO
   TS
CP0396699
1-(1H-indazol-6-yl)-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C15H18N6S
 1
1
IC50 = 381 nM
   TI
   LI
   LO
   TS
CP0407302
1-(2,3-dihydro-1-benzofuran-6-yl)-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C16H20N4OS
 1
1
IC50 = 405 nM
   TI
   LI
   LO
   TS
CP0525835
1-(2,3-dihydro-1-benzofuran-5-yl)-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C16H20N4OS
 1
1
IC50 = 437 nM
   TI
   LI
   LO
   TS
CP0396697
1-[3-(5-methylimidazol-1-yl)propyl]-3-pyridin-2-ylthiourea
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C13H17N5S
 1
1
IC50 = 453 nM
   TI
   LI
   LO
   TS
CP0407467
1-(3-methylbenzimidazol-5-yl)-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C16H20N6S
 1
1
IC50 = 461 nM
   TI
   LI
   LO
   TS
CP0407468
1-(3H-benzimidazol-5-yl)-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C15H18N6S
 1
1
IC50 = 463 nM
   TI
   LI
   LO
   TS
CP0407466
1-(1,3-benzoxazol-5-yl)-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C15H17N5OS
 1
1
IC50 = 475 nM
   TI
   LI
   LO
   TS
CP0508662
1-(3,4-dihydro-2H-chromen-7-yl)-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C17H22N4OS
 1
1
IC50 = 479 nM
   TI
   LI
   LO
   TS
CP0527526
1-[3-(5-methylimidazol-1-yl)propyl]-3-(5-oxo-7,8-dihydro-6H-naphthalen-2-yl)thiourea
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C18H22N4OS
 1
1
IC50 = 482 nM
   TI
   LI
   LO
   TS
CP0396698
1-(1,3-benzothiazol-6-yl)-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C15H17N5S2
 1
1
IC50 = 488 nM
   TI
   LI
   LO
   TS
CP0482356
1-(3,4-dihydro-2H-1,4-benzoxazin-6-yl)-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C16H21N5OS
 1
1
IC50 = 492 nM
   TI
   LI
   LO
   TS
CP0508657
1-isoquinolin-3-yl-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C17H19N5S
 1
1
IC50 = 518 nM
   TI
   LI
   LO
   TS
CP0397493
1-(5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C18H24N4OS
 1
1
IC50 = 519 nM
   TI
   LI
   LO
   TS
CP0397491
1-(2-methyl-1,3-benzoxazol-5-yl)-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C16H19N5OS
 1
1
IC50 = 524 nM
   TI
   LI
   LO
   TS
CP0527525
1-isoquinolin-5-yl-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C17H19N5S
 1
1
IC50 = 546 nM
   TI
   LI
   LO
   TS
CP0508659
1-(1-methylbenzimidazol-5-yl)-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C16H20N6S
 1
1
IC50 = 711 nM
   TI
   LI
   LO
   TS
CP0508656
1-[3-(5-methylimidazol-1-yl)propyl]-3-quinolin-7-ylthiourea
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C17H19N5S
 1
1
IC50 = 768 nM
   TI
   LI
   LO
   TS
CP0540386
1-[3-(5-methylimidazol-1-yl)propyl]-3-(8-oxo-6,7-dihydro-5H-naphthalen-2-yl)thiourea
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C18H22N4OS
 1
1
IC50 = 788 nM
   TI
   LI
   LO
   TS
CP0508661
1-(8-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C18H24N4OS
 1
1
IC50 = 812 nM
   TI
   LI
   LO
   TS
CP0407301
1-(1,3-benzoxazol-6-yl)-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C15H17N5OS
 1
1
IC50 = 1070 nM
   TI
   LI
   LO
   TS
CP0423026
1-(3,4-dihydro-2H-1,4-benzoxazin-7-yl)-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C16H21N5OS
 1
1
IC50 = 1070 nM
   TI
   LI
   LO
   TS
CP0501318
1-(1,3-benzothiazol-5-yl)-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C15H17N5S2
 1
1
IC50 = 1220 nM
   TI
   LI
   LO
   TS
CP0396700
1-[3-(5-methylimidazol-1-yl)propyl]-3-(1-methylindol-6-yl)thiourea
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C17H21N5S
 1
1
IC50 = 1613 nM
   TI
   LI
   LO
   TS
CP0489522
1-[3-(5-methylimidazol-1-yl)propyl]-3-quinoxalin-6-ylthiourea
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C16H18N6S
 1
1
IC50 = 3050 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0103701
1-[4-[4-(2-aminopyridin-4-yl)butoxy]-3-methoxyphenyl]-3-[3-(5-methylimidazol-1-yl)propyl]thiourea
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C24H32N6O2S
 1
1 IC50 = 4.5 nM
CP0533267
2-fluoro-5-[2-[4-(4-methyl-1,2,4-triazol-3-yl)piperidin-1-yl]pyridin-3-yl]pyridine
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C18H19FN6
 1
1 IC50 = 16.7 nM
CP0206338
US8486940, 13
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C19H20N4O2
 3
1 IC50 = 29 nM
2 IC50 = 30200 nM
3 Ki = 7250 nM
CP0370024
1-(3,4-Dimethoxyphenyl)-3-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea
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C16H22N4O2S
 1
1 IC50 = 29.2 nM
CP0251885
US9181233, 67
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C18H16N4O2S2
 1
1 IC50 = 47.9 nM
CP0416941
2-(4-fluorophenyl)-N-[3-(4-methylimidazol-1-yl)propyl]aniline
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C19H20FN3
 1
1 IC50 = 118 nM
CP0477452
US9512082, 1
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C16H22N4O3
 1
1 IC50 = 162 nM
Clinical Information about the Protein
Target 1 ( Glutaminyl cyclase (QPCT) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Dementia [ICD-11: 6D80-6D86]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 PQ-912 Phase 2
Dementia