QPCTL
gene geneOn this page
Also known as FLJ20084
Summary
QPCTL (glutaminyl-peptide cyclotransferase like, HGNC:25952) is a protein-coding gene on chromosome 19q13.32, encoding Glutaminyl-peptide cyclotransferase-like protein (Q9NXS2). Responsible for the biosynthesis of pyroglutamyl peptides.
Enables glutaminyl-peptide cyclotransferase activity and zinc ion binding activity. Located in Golgi apparatus.
Source: NCBI Gene 54814 — RefSeq curated summary.
At a glance
- GWAS associations: 22
- Clinical variants (ClinVar): 91 total
- Druggable target: yes — 2 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_017659
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:25952 |
| Approved symbol | QPCTL |
| Name | glutaminyl-peptide cyclotransferase like |
| Location | 19q13.32 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | FLJ20084 |
| Ensembl gene | ENSG00000011478 |
| Ensembl biotype | protein_coding |
| Entrez | 54814 |
Gene structure
Transcript identifiers
Ensembl transcripts: 8 — 5 nonsense_mediated_decay, 2 protein_coding, 1 retained_intron
ENST00000012049, ENST00000366382, ENST00000591606, ENST00000592769, ENST00000677024, ENST00000677542, ENST00000678102, ENST00000678862
RefSeq mRNA: 2 — MANE Select: NM_017659
NM_001163377, NM_017659
CCDS: CCDS12672, CCDS54282
Canonical transcript exons
ENST00000012049 — 7 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000358959 | 45693413 | 45693556 |
| ENSE00000713040 | 45695437 | 45695718 |
| ENSE00000713044 | 45698801 | 45698900 |
| ENSE00000713047 | 45701798 | 45701914 |
| ENSE00000858251 | 45692666 | 45692910 |
| ENSE00003574310 | 45698547 | 45698699 |
| ENSE00003851017 | 45702904 | 45703987 |
Expression profiles
Bgee: expression breadth ubiquitous, 157 present calls, max score 83.98.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 15.4934 / max 93.4543, expressed in 1795 samples.
FANTOM5 promoters (2 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 176502 | 15.2682 | 1795 |
| 176503 | 0.2252 | 110 |
Top tissues by expression
251 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| stromal cell of endometrium | CL:0002255 | 83.98 | gold quality |
| bone marrow cell | CL:0002092 | 82.63 | gold quality |
| mucosa of transverse colon | UBERON:0004991 | 81.19 | gold quality |
| left adrenal gland cortex | UBERON:0035825 | 79.91 | gold quality |
| right lobe of thyroid gland | UBERON:0001119 | 79.77 | gold quality |
| right lobe of liver | UBERON:0001114 | 79.51 | gold quality |
| right adrenal gland cortex | UBERON:0035827 | 79.43 | gold quality |
| right adrenal gland | UBERON:0001233 | 79.28 | gold quality |
| left adrenal gland | UBERON:0001234 | 79.25 | gold quality |
| left lobe of thyroid gland | UBERON:0001120 | 79.04 | gold quality |
| popliteal artery | UBERON:0002250 | 78.61 | gold quality |
| tibial artery | UBERON:0007610 | 78.60 | gold quality |
| body of stomach | UBERON:0001161 | 78.59 | gold quality |
| transverse colon | UBERON:0001157 | 78.51 | gold quality |
| body of pancreas | UBERON:0001150 | 78.33 | gold quality |
| cerebellar hemisphere | UBERON:0002245 | 77.98 | gold quality |
| adenohypophysis | UBERON:0002196 | 77.97 | gold quality |
| cerebellar cortex | UBERON:0002129 | 77.88 | gold quality |
| spleen | UBERON:0002106 | 77.78 | gold quality |
| right ovary | UBERON:0002118 | 77.70 | gold quality |
| Brodmann (1909) area 9 | UBERON:0013540 | 77.62 | gold quality |
| aorta | UBERON:0000947 | 77.60 | gold quality |
| left ovary | UBERON:0002119 | 77.59 | gold quality |
| upper lobe of left lung | UBERON:0008952 | 77.59 | gold quality |
| minor salivary gland | UBERON:0001830 | 77.49 | gold quality |
| right hemisphere of cerebellum | UBERON:0014890 | 77.20 | gold quality |
| thyroid gland | UBERON:0002046 | 77.13 | gold quality |
| adrenal cortex | UBERON:0001235 | 77.06 | gold quality |
| apex of heart | UBERON:0002098 | 77.05 | gold quality |
| ascending aorta | UBERON:0001496 | 76.81 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 3.24 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
30 targeting QPCTL, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-3613-3P | 100.00 | 76.36 | 7965 |
| HSA-MIR-4425 | 100.00 | 67.59 | 1049 |
| HSA-MIR-7110-3P | 100.00 | 73.18 | 2486 |
| HSA-MIR-371B-5P | 99.99 | 75.34 | 4759 |
| HSA-MIR-373-5P | 99.98 | 75.36 | 4753 |
| HSA-MIR-616-5P | 99.98 | 75.58 | 4775 |
| HSA-MIR-3681-3P | 99.88 | 70.46 | 2254 |
| HSA-MIR-4728-5P | 99.85 | 69.39 | 4718 |
| HSA-MIR-6785-5P | 99.82 | 68.68 | 4428 |
| HSA-MIR-3133 | 99.81 | 70.92 | 3506 |
| HSA-MIR-149-3P | 99.72 | 68.22 | 3963 |
| HSA-MIR-6883-5P | 99.69 | 68.05 | 3785 |
| HSA-MIR-7106-5P | 99.53 | 67.47 | 3574 |
| HSA-MIR-4284 | 99.36 | 65.25 | 1293 |
| HSA-MIR-504-3P | 99.30 | 67.18 | 1745 |
| HSA-MIR-6799-5P | 99.14 | 65.72 | 2093 |
| HSA-MIR-520G-3P | 98.91 | 67.38 | 1914 |
| HSA-MIR-520H | 98.91 | 67.38 | 1914 |
| HSA-MIR-5089-5P | 98.45 | 66.06 | 1388 |
| HSA-MIR-6516-5P | 98.42 | 70.19 | 1551 |
| HSA-MIR-4773 | 98.35 | 67.30 | 1710 |
| HSA-MIR-340-3P | 98.11 | 68.25 | 679 |
| HSA-MIR-6827-3P | 98.08 | 72.27 | 651 |
| HSA-MIR-6747-3P | 97.73 | 64.84 | 1596 |
| HSA-MIR-585-5P | 97.54 | 69.02 | 955 |
| HSA-MIR-4776-5P | 97.14 | 66.63 | 405 |
| HSA-MIR-339-5P | 96.73 | 66.01 | 820 |
| HSA-MIR-6888-5P | 95.89 | 63.78 | 831 |
| HSA-MIR-3193 | 92.99 | 64.93 | 116 |
| HSA-MIR-6825-3P | 88.51 | 66.17 | 71 |
Literature-anchored findings (GeneRIF, showing 4)
- genetic association studies in Danish population: Quantitative metabolic phenotypes in obesity are associated with SNP in various genes: QPCTL (rs2287019) is associated with body mass index and increased insulinogenic index. (PMID:21953277)
- QPCTL is critical for pyroglutamate formation on CD47 at the SIRPalpha binding site shortly after biosynthesis. (PMID:30833751)
- Senescent cells suppress macrophage-mediated corpse removal via upregulation of the CD47-QPCT/L axis. (PMID:36459066)
- Deciphering the role of QPCTL in glioma progression and cancer immunotherapy. (PMID:37063864)
Cross-species orthologs
9 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | qpctla | ENSDARG00000061691 |
| danio_rerio | qpctlb | ENSDARG00000062293 |
| mus_musculus | Qpctl | ENSMUSG00000030407 |
| rattus_norvegicus | Qpctl | ENSRNOG00000015413 |
| drosophila_melanogaster | CG6168 | FBGN0036154 |
| drosophila_melanogaster | isoQC | FBGN0036999 |
| drosophila_melanogaster | QC | FBGN0052412 |
| drosophila_melanogaster | CG32413 | FBGN0052413 |
| caenorhabditis_elegans | WBGENE00010418 |
Paralogs (1): QPCT (ENSG00000115828)
Protein
Protein identifiers
Glutaminyl-peptide cyclotransferase-like protein — Q9NXS2 (reviewed: Q9NXS2)
Alternative names: Golgi-resident glutaminyl-peptide cyclotransferase, isoQC
All UniProt accessions (4): Q9NXS2, A0A7I2V353, A0A7I2V5X1, K7EQG1
UniProt curated annotations — full annotation on UniProt →
Function. Responsible for the biosynthesis of pyroglutamyl peptides.
Subcellular location. Golgi apparatus membrane.
Similarity. Belongs to the glutaminyl-peptide cyclotransferase family.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| Q9NXS2-1 | 1 | yes |
| Q9NXS2-3 | 2 |
RefSeq proteins (2): NP_001156849, NP_060129* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR007484 | Peptidase_M28 | Domain |
| IPR037457 | M28_QC | Domain |
| IPR040234 | QC/QCL | Family |
Pfam: PF04389
Enzyme classification (BRENDA):
- EC 2.3.2.5 — glutaminyl-peptide cyclotransferase (BRENDA: 29 organisms, 258 substrates, 720 inhibitors, 348 Km, 331 kcat entries)
Substrate kinetics (BRENDA)
145 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| GLN-GLN | 0.044–29.53 | 22 |
| GLN-NH2 | 0.401–7.15 | 11 |
| GLN-2-NAPHTHYLAMIDE | 0.058–1.1 | 10 |
| L-GLUTAMINE TERT-BUTYL ESTER | 0.379–1.3 | 10 |
| GLN-GLU | 0.094–0.61 | 7 |
| L-GLN-2-NAPHTHYLAMIDE | 0.028–0.5 | 7 |
| GLN-ALA | 0.143–1.3 | 6 |
| GLN-GLY | 0.16–1.88 | 6 |
| H-GLN-BETA-NAPHTHYLAMIDE | 0.028–0.17 | 5 |
| H-GLN-GLN-OH | 0.053–1.5 | 5 |
| H-GLN-GLY-OH | 0.424–7.1 | 5 |
| L-GLN-7-AMIDO-4-METHYLCOUMARIN | 0.048–0.3 | 5 |
| L-GLN-L-GLN | 0.053–20.4 | 5 |
| L-GLN-L-GLU | 0.265–4.2 | 5 |
| GLN-ARG-GLY-ILE-NH2 | 0.065–0.143 | 4 |
Catalyzed reactions (Rhea), 1 shown:
- N-terminal L-glutaminyl-[peptide] = N-terminal 5-oxo-L-prolyl-[peptide] + NH4(+) (RHEA:23652)
UniProt features (40 total): helix 12, strand 11, turn 4, sequence conflict 3, binding site 3, active site 2, chain 1, transmembrane region 1, disulfide bond 1, splice variant 1, sequence variant 1
Structure
Experimental structures (PDB)
7 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 3PB6 | X-RAY DIFFRACTION | 1.05 |
| 3PB9 | X-RAY DIFFRACTION | 1.12 |
| 3PB4 | X-RAY DIFFRACTION | 1.13 |
| 3PB8 | X-RAY DIFFRACTION | 1.13 |
| 3PB7 | X-RAY DIFFRACTION | 1.4 |
| 8XFV | X-RAY DIFFRACTION | 3.13 |
| 8XGA | X-RAY DIFFRACTION | 3.54 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q9NXS2-F1 | 89.12 | 0.78 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Catalytic / active sites (2): 225 (proton acceptor); 269 (proton acceptor)
Ligand- & substrate-binding residues (3): 186; 226; 351
Disulfide bonds (1): 167–191
Function
Pathways and Gene Ontology
Reactome pathways
0 pathways
MSigDB gene sets: 67 (showing top):
TGCGCANK_UNKNOWN, IVANOVA_HEMATOPOIESIS_LATE_PROGENITOR, MORI_PLASMA_CELL_UP, MARSON_BOUND_BY_FOXP3_UNSTIMULATED, GOMF_ACYLTRANSFERASE_ACTIVITY, GOMF_AMINOACYLTRANSFERASE_ACTIVITY, MCBRYAN_PUBERTAL_BREAST_6_7WK_UP, BAKKER_FOXO3_TARGETS_DN, SRC_UP.V1_UP, BARX1_TARGET_GENES, CEBPZ_TARGET_GENES, DLX4_TARGET_GENES, E2F2_TARGET_GENES, FOXD2_TARGET_GENES, HOXC6_TARGET_GENES
GO Biological Process (1): peptidyl-pyroglutamic acid biosynthetic process, using glutaminyl-peptide cyclotransferase (GO:0017186)
GO Molecular Function (6): zinc ion binding (GO:0008270), glutaminyl-peptide cyclotransferase activity (GO:0016603), protein binding (GO:0005515), transferase activity (GO:0016740), acyltransferase activity (GO:0016746), metal ion binding (GO:0046872)
GO Cellular Component (3): Golgi membrane (GO:0000139), Golgi apparatus (GO:0005794), membrane (GO:0016020)
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| peptidyl-glutamine modification | 1 |
| transition metal ion binding | 1 |
| aminoacyltransferase activity | 1 |
| catalytic activity, acting on a protein | 1 |
| binding | 1 |
| catalytic activity | 1 |
| transferase activity | 1 |
| cation binding | 1 |
| Golgi apparatus | 1 |
| bounding membrane of organelle | 1 |
| cytoplasm | 1 |
| endomembrane system | 1 |
| intracellular membrane-bounded organelle | 1 |
| cellular anatomical structure | 1 |
Protein interactions and networks
STRING
770 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| QPCTL | GIPR | P48546 | 749 |
| QPCTL | GNPDA2 | Q8TDQ7 | 635 |
| QPCTL | SEC16B | Q96JE7 | 609 |
| QPCTL | V9GXZ4 | V9GXZ4 | 609 |
| QPCTL | TNNI3K | Q59H18 | 608 |
| QPCTL | TMEM160 | Q9NX00 | 605 |
| QPCTL | MTIF3 | Q9H2K0 | 603 |
| QPCTL | DNAJC27 | Q9NZQ0 | 597 |
| QPCTL | NUDT3 | O95989 | 592 |
| QPCTL | TMEM18 | Q96B42 | 581 |
| QPCTL | KCTD15 | Q96SI1 | 578 |
| QPCTL | ZNF608 | Q9ULD9 | 571 |
| QPCTL | POC5 | Q8NA72 | 545 |
| QPCTL | MTCH2 | Q9Y6C9 | 540 |
| QPCTL | SH2B1 | Q9NRF2 | 539 |
IntAct
83 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| SLC39A5 | FAM171A2 | psi-mi:“MI:0914”(association) | 0.640 |
| DCAF7 | PFDN6 | psi-mi:“MI:0914”(association) | 0.570 |
| PEX19 | FAM20B | psi-mi:“MI:0914”(association) | 0.530 |
| XPO1 | psi-mi:“MI:0914”(association) | 0.530 | |
| QPCTL | Dlg4 | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| GPC1 | GANAB | psi-mi:“MI:0915”(physical association) | 0.400 |
| OTUB1 | psi-mi:“MI:0914”(association) | 0.350 | |
| OTUB1 | EPM2A | psi-mi:“MI:0914”(association) | 0.350 |
| ESYT2 | psi-mi:“MI:0914”(association) | 0.350 | |
| E5 | ESYT2 | psi-mi:“MI:0914”(association) | 0.350 |
| PGRMC1 | psi-mi:“MI:0914”(association) | 0.350 | |
| SNAP23 | psi-mi:“MI:0914”(association) | 0.350 | |
| HAX1 | psi-mi:“MI:0914”(association) | 0.350 | |
| BVLF1 | VWA8 | psi-mi:“MI:0914”(association) | 0.350 |
| HA | ESYT2 | psi-mi:“MI:0914”(association) | 0.350 |
| M | PGRMC1 | psi-mi:“MI:0914”(association) | 0.350 |
| M | NPEPPSL1 | psi-mi:“MI:0914”(association) | 0.350 |
| PB1 | HAX1 | psi-mi:“MI:0914”(association) | 0.350 |
| PB2 | ESYT2 | psi-mi:“MI:0914”(association) | 0.350 |
| NS1 | HAX1 | psi-mi:“MI:0914”(association) | 0.350 |
| M2 | ESYT2 | psi-mi:“MI:0914”(association) | 0.350 |
| COX15 | SNRPGP15 | psi-mi:“MI:0914”(association) | 0.350 |
| L1TD1 | MYO1C | psi-mi:“MI:0914”(association) | 0.350 |
| ESR1 | ESYT2 | psi-mi:“MI:0914”(association) | 0.350 |
| CAMK1D | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (111): QPCTL (Affinity Capture-MS), QPCTL (Affinity Capture-MS), QPCTL (Affinity Capture-MS), QPCTL (Affinity Capture-MS), QPCTL (Affinity Capture-MS), QPCTL (Affinity Capture-MS), QPCTL (Affinity Capture-MS), QPCTL (Affinity Capture-MS), QPCTL (Affinity Capture-MS), QPCTL (Affinity Capture-RNA), QPCTL (Affinity Capture-MS), QPCTL (Affinity Capture-MS), QPCTL (Affinity Capture-MS), QPCTL (Affinity Capture-MS), QPCTL (Affinity Capture-MS)
ESM2 similar proteins: A0JND9, D3YTS9, O19058, O35795, O55026, O75173, P08648, P11117, P17405, P20611, P21217, P24638, P29376, P56433, Q04519, Q0P5F0, Q0V8G3, Q0VD19, Q11128, Q11131, Q32M88, Q4R5N9, Q4R942, Q5MY95, Q5NVF6, Q5RFQ8, Q62994, Q63148, Q6IY74, Q8BH73, Q8HYJ3, Q8HYJ4, Q8HYJ5, Q8HYJ7, Q8HZR3, Q8K1S1, Q8N135, Q923W9, Q9BZG2, Q9H3T2
Diamond homologs: A7ISW1, A7ISW2, B7QK46, P0CV92, P43599, Q0V8G3, Q16769, Q28120, Q4R942, Q54B14, Q86PD7, Q8BH73, Q90YA8, Q9CYK2, Q9NXS2, Q9VRQ9, Q9YIB5
SIGNOR signaling
0 interactions.
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 98 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.
Reactome pathways:
| Pathway | Partners | Fold | FDR |
|---|---|---|---|
| Metal ion SLC transporters | 7 | 59.3× | 3e-09 |
| VEGFR2 mediated cell proliferation | 5 | 40.2× | 2e-05 |
| R-HSA-425366 | 6 | 15.3× | 1e-04 |
| Regulation of RAS by GAPs | 5 | 13.6× | 8e-04 |
| MAPK6/MAPK4 signaling | 7 | 13.4× | 6e-05 |
| Ca2+ pathway | 5 | 12.6× | 1e-03 |
| ESR-mediated signaling | 6 | 10.8× | 6e-04 |
| Signaling by Nuclear Receptors | 5 | 7.2× | 6e-03 |
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| zinc ion transmembrane transport | 9 | 83.2× | 5e-13 |
| intracellular monoatomic cation homeostasis | 5 | 73.9× | 1e-06 |
| intracellular zinc ion homeostasis | 9 | 57.0× | 1e-11 |
| insulin receptor signaling pathway | 5 | 14.6× | 2e-03 |
| MAPK cascade | 6 | 12.1× | 1e-03 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
91 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 73 |
| Likely benign | 3 |
| Benign | 1 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
1441 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 19:45692877:GAC:G | donor_gain | 1.0000 |
| 19:45698545:A:AG | acceptor_gain | 1.0000 |
| 19:45698546:G:GG | acceptor_gain | 1.0000 |
| 19:45698578:T:TA | acceptor_gain | 1.0000 |
| 19:45698694:GC:G | donor_gain | 1.0000 |
| 19:45698698:TT:T | donor_gain | 1.0000 |
| 19:45698700:G:GG | donor_gain | 1.0000 |
| 19:45701780:A:AG | acceptor_gain | 1.0000 |
| 19:45701780:AATC:A | acceptor_gain | 1.0000 |
| 19:45701781:A:G | acceptor_gain | 1.0000 |
| 19:45701781:ATC:A | acceptor_gain | 1.0000 |
| 19:45701783:C:CA | acceptor_gain | 1.0000 |
| 19:45701790:A:AG | acceptor_gain | 1.0000 |
| 19:45701793:TCCAG:T | acceptor_gain | 1.0000 |
| 19:45701794:CCAG:C | acceptor_gain | 1.0000 |
| 19:45701795:CA:C | acceptor_loss | 1.0000 |
| 19:45701796:A:AG | acceptor_gain | 1.0000 |
| 19:45701797:G:C | acceptor_gain | 1.0000 |
| 19:45701797:G:GT | acceptor_gain | 1.0000 |
| 19:45701797:GA:G | acceptor_gain | 1.0000 |
| 19:45701797:GAGA:G | acceptor_gain | 1.0000 |
| 19:45701797:GAGAA:G | acceptor_gain | 1.0000 |
| 19:45701842:G:GT | donor_gain | 1.0000 |
| 19:45701884:G:GT | donor_gain | 1.0000 |
| 19:45701912:GAG:G | donor_gain | 1.0000 |
| 19:45701913:AG:A | donor_loss | 1.0000 |
| 19:45701914:GGTA:G | donor_loss | 1.0000 |
| 19:45701915:G:GA | donor_loss | 1.0000 |
| 19:45702902:AGG:A | acceptor_gain | 1.0000 |
| 19:45702903:GGG:G | acceptor_gain | 1.0000 |
AlphaMissense
2415 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 19:45701887:G:C | D326H | 0.993 |
| 19:45695586:C:G | C167W | 0.991 |
| 19:45698823:T:C | L270P | 0.991 |
| 19:45695645:C:G | S187W | 0.989 |
| 19:45702963:G:C | D355H | 0.989 |
| 19:45701799:G:C | E296D | 0.988 |
| 19:45701799:G:T | E296D | 0.988 |
| 19:45701888:A:T | D326V | 0.988 |
| 19:45702936:T:C | F346L | 0.988 |
| 19:45702938:C:A | F346L | 0.988 |
| 19:45702938:C:G | F346L | 0.988 |
| 19:45695473:T:A | W130R | 0.987 |
| 19:45695473:T:C | W130R | 0.987 |
| 19:45695584:T:C | C167R | 0.987 |
| 19:45695587:C:G | H168D | 0.987 |
| 19:45698829:G:A | G272E | 0.987 |
| 19:45701807:T:C | L299P | 0.987 |
| 19:45701891:A:T | D327V | 0.987 |
| 19:45698606:G:C | W231C | 0.986 |
| 19:45698606:G:T | W231C | 0.986 |
| 19:45701798:A:T | E296V | 0.986 |
| 19:45701855:T:C | F315S | 0.986 |
| 19:45695658:T:G | C191W | 0.985 |
| 19:45698575:T:C | F221S | 0.985 |
| 19:45698590:A:T | E226V | 0.985 |
| 19:45698828:G:A | G272R | 0.985 |
| 19:45698828:G:C | G272R | 0.985 |
| 19:45701890:G:C | D327H | 0.985 |
| 19:45701902:T:C | F331L | 0.985 |
| 19:45701903:T:C | F331S | 0.985 |
dbSNP variants (sampled 300 via entrez): RS1000176536 (19:45699279 C>A,T), RS1000251542 (19:45691305 A>G), RS1000395257 (19:45702938 C>T), RS1000412954 (19:45696368 G>A), RS1000904139 (19:45691967 T>C,G), RS1001201233 (19:45695901 A>T), RS1001582938 (19:45696016 G>T), RS1002181467 (19:45701607 A>G), RS1002573630 (19:45704365 A>AG), RS1002865639 (19:45691747 C>T), RS1003156464 (19:45698927 C>T), RS1003245489 (19:45695033 C>T), RS1003264011 (19:45700757 G>A,T), RS1003270050 (19:45694718 C>T), RS1003889087 (19:45691284 C>T)
Disease associations
OMIM: gene `` | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
22 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST000830_7 | Body mass index | 2.000000e-16 |
| GCST001415_4 | Body mass index | 6.000000e-14 |
| GCST001521_39 | Subcutaneous adipose tissue | 1.000000e-06 |
| GCST002461_12 | Body mass index | 3.000000e-12 |
| GCST002783_276 | Body mass index | 2.000000e-18 |
| GCST002783_40 | Body mass index | 9.000000e-10 |
| GCST002783_631 | Body mass index | 5.000000e-18 |
| GCST002783_73 | Body mass index | 3.000000e-12 |
| GCST004064_21 | Waist-hip ratio | 2.000000e-07 |
| GCST004064_56 | Waist-hip ratio | 4.000000e-09 |
| GCST004065_35 | Waist circumference | 4.000000e-09 |
| GCST004065_39 | Waist circumference | 2.000000e-14 |
| GCST004065_44 | Waist circumference | 6.000000e-08 |
| GCST004495_89 | BMI (adjusted for smoking behaviour) | 3.000000e-06 |
| GCST004495_90 | BMI (adjusted for smoking behaviour) | 7.000000e-09 |
| GCST004497_32 | Body mass index (joint analysis main effects and smoking interaction) | 1.000000e-07 |
| GCST004499_96 | BMI in non-smokers | 5.000000e-06 |
| GCST006585_982 | Blood protein levels | 5.000000e-19 |
| GCST006802_25 | Body mass index | 8.000000e-11 |
| GCST007612_3 | Chronic obstructive pulmonary disease or coronary artery disease (pleiotropy) | 1.000000e-08 |
| GCST010136_35 | Fruit consumption | 1.000000e-11 |
| GCST011569_9 | Pancreatic beta-cell glucose sensitivity | 3.000000e-09 |
EFO canonical traits (5, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004340 | body mass index |
| EFO:0004343 | waist-hip ratio |
| EFO:0004318 | smoking behavior |
| EFO:0008111 | diet measurement |
| EFO:0006842 | diabetes mellitus biomarker |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL3638349 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
2 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 23,623 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL151 | LUTEOLIN | 2 | 23,523 |
| CHEMBL3659477 | VAROGLUTAMSTAT | 2 | 100 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: enzyme — M28: Aminopeptidase Y
Most potent curated ligand interactions (5 total), top 5:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| QP5038 | Inhibition | 8.48 | pIC50 |
| QP5020 | Inhibition | 8.19 | pIC50 |
| BI-43 | Inhibition | 7.4 | pIC50 |
| SEN177 | Inhibition | 6.49 | pIC50 |
| varoglutamstat | Inhibition | 6.01 | pIC50 |
Binding affinities (BindingDB)
54 measured of 54 human assays (54 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| 2-[4-fluoro-4-(4-methyl-1,2,4-triazol-3-yl)piperidin-1-yl]-3-(6-fluoro-3-pyridinyl)-5-(2-hydroxypropan-2-yl)benzonitrile | IC50 | 1 nM | US-20250250252: PIPERIDINYLBENZONITRILE DERIVATIVES AS INHIBITORS OF GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE AND GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE LIKE PROTEIN |
| 2-[4-fluoro-4-(4-methyl-1,2,4-triazol-3-yl)piperidin-1-yl]-3-(6-fluoro-3-pyridinyl)-5-(2-methyl-1,3-oxazol-5-yl)benzonitrile | IC50 | 2 nM | US-20250250252: PIPERIDINYLBENZONITRILE DERIVATIVES AS INHIBITORS OF GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE AND GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE LIKE PROTEIN |
| 5-(1,3-dimethylpyrazol-4-yl)-2-[4-fluoro-4-(4-methyl-1,2,4-triazol-3-yl)piperidin-1-yl]-3-(6-fluoro-3-pyridinyl)benzonitrile | IC50 | 2 nM | US-20250250252: PIPERIDINYLBENZONITRILE DERIVATIVES AS INHIBITORS OF GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE AND GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE LIKE PROTEIN |
| 2-[4-fluoro-4-(4-methyl-1,2,4-triazol-3-yl)piperidin-1-yl]-3-(6-fluoro-3-pyridinyl)-5-(1-methylpyrazol-4-yl)benzonitrile | IC50 | 2 nM | US-20250250252: PIPERIDINYLBENZONITRILE DERIVATIVES AS INHIBITORS OF GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE AND GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE LIKE PROTEIN |
| 2-[4-fluoro-4-(4-methyl-1,2,4-triazol-3-yl)piperidin-1-yl]-3-(6-fluoro-3-pyridinyl)-5-pyridazin-4-ylbenzonitrile | IC50 | 2 nM | US-20250250252: PIPERIDINYLBENZONITRILE DERIVATIVES AS INHIBITORS OF GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE AND GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE LIKE PROTEIN |
| 2-[4-fluoro-4-(4-methyl-1,2,4-triazol-3-yl)piperidin-1-yl]-3-(6-fluoro-3-pyridinyl)-5-pyridin-3-ylbenzonitrile | IC50 | 3 nM | US-20250250252: PIPERIDINYLBENZONITRILE DERIVATIVES AS INHIBITORS OF GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE AND GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE LIKE PROTEIN |
| 2-[4-fluoro-4-(4-methyl-1,2,4-triazol-3-yl)piperidin-1-yl]-3-(6-fluoro-3-pyridinyl)-5-(2-methylpyrimidin-5-yl)benzonitrile | IC50 | 3 nM | US-20250250252: PIPERIDINYLBENZONITRILE DERIVATIVES AS INHIBITORS OF GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE AND GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE LIKE PROTEIN |
| 2-[4-fluoro-4-(4-methyl-1,2,4-triazol-3-yl)piperidin-1-yl]-3-(6-fluoro-3-pyridinyl)-5-[2-(trifluoromethyl)pyrimidin-5-yl]benzonitrile | IC50 | 3 nM | US-20250250252: PIPERIDINYLBENZONITRILE DERIVATIVES AS INHIBITORS OF GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE AND GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE LIKE PROTEIN |
| 2-[4-fluoro-4-(4-methyl-1,2,4-triazol-3-yl)piperidin-1-yl]-3-(6-fluoro-3-pyridinyl)-5-(1,3,5-trimethylpyrazol-4-yl)benzonitrile | IC50 | 4 nM | US-20250250252: PIPERIDINYLBENZONITRILE DERIVATIVES AS INHIBITORS OF GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE AND GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE LIKE PROTEIN |
| 2-(3H-benzimidazol-5-yl)-5-[(3,4-dimethoxyphenyl)sulfanylmethyl]-1,3,4-thiadiazole | KI | 10 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| (E)-1-N’-cyclohexyl-1-N-[4-(5-methylimidazol-1-yl)butyl]-2-nitroethene-1,1-diamine | KI | 11 nM | US-8772508: Inhibitors of glutaminyl cyclase |
| N’-[3-(5-methylimidazol-1-yl)propyl]-2-nitro-N-[4-(trifluoromethyl)phenyl]ethanimidamide | KI | 34 nM | US-8772508: Inhibitors of glutaminyl cyclase |
| 2-(3H-benzimidazol-5-yl)-5-[2-(3-methoxyphenyl)ethyl]-1,3,4-thiadiazole | KI | 40 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| N’-[3-(5-methylimidazol-1-yl)propyl]-N-naphthalen-1-yl-2-nitroethanimidamide | KI | 41 nM | US-8772508: Inhibitors of glutaminyl cyclase |
| 2-(3H-benzimidazol-5-yl)-5-[2-(3-chloro-4-methoxyphenyl)ethyl]-1,3,4-thiadiazole | KI | 50 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| N-(4-chlorophenyl)-N’-[3-(5-methylimidazol-1-yl)propyl]-2-nitroethanimidamide | KI | 51 nM | US-8772508: Inhibitors of glutaminyl cyclase |
| (E)-1-N’-(2,4-dimethoxyphenyl)-1-N-[3-(5-methylimidazol-1-yl)propyl]-2-nitroethene-1,1-diamine | KI | 55 nM | US-8772508: Inhibitors of glutaminyl cyclase |
| 2-(3H-benzimidazol-5-yl)-5-[2-(3,4-dimethoxyphenyl)ethyl]-1,3,4-thiadiazole | KI | 60 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| 2-(3H-benzimidazol-5-yl)-5-[2-(1,3-benzodioxol-5-yl)ethyl]-1,3,4-thiadiazole | KI | 60 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| (E)-1-N’-(1,3-benzodioxol-5-yl)-1-N-[3-(5-methylimidazol-1-yl)propyl]-2-nitroethene-1,1-diamine | KI | 67 nM | US-8772508: Inhibitors of glutaminyl cyclase |
| N-(2,3-dihydro-1,4-benzodioxin-6-yl)-N’-[3-(5-methylimidazol-1-yl)propyl]-2-nitroethanimidamide | KI | 67 nM | US-8772508: Inhibitors of glutaminyl cyclase |
| (E)-1-N’-(3,4-dimethoxyphenyl)-1-N-[3-(5-methylimidazol-1-yl)propyl]-2-nitroethene-1,1-diamine | KI | 76 nM | US-8772508: Inhibitors of glutaminyl cyclase |
| 6-[4-[(4-phenoxyphenyl)methyl]-1,2,4-triazol-3-yl]-1H-benzimidazole | KI | 80 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| 2-(3H-benzimidazol-5-yl)-5-[2-(4-methylsulfanylphenyl)ethyl]-1,3,4-thiadiazole | KI | 80 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| 2-(3H-benzimidazol-5-yl)-5-[2-(3,4,5-trimethoxyphenyl)ethyl]-1,3,4-thiadiazole | KI | 80 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| 2-(3H-benzimidazol-5-yl)-5-[2-(2,5-dimethoxyphenyl)ethyl]-1,3,4-thiadiazole | KI | 80 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| 6-[1-[2-(4-methoxyphenyl)ethyl]triazol-4-yl]-1H-benzimidazole | KI | 80 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| N-cyclohexyl-N’-[3-(5-methylimidazol-1-yl)propyl]-2-nitroethanimidamide | KI | 80 nM | US-8772508: Inhibitors of glutaminyl cyclase |
| 2-(3H-benzimidazol-5-yl)-5-[2-(2,3-dimethoxyphenyl)ethyl]-1,3,4-thiadiazole | KI | 90 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| (E)-1-N-[3-(5-methylimidazol-1-yl)propyl]-2-nitro-1-N’-(3,4,5-trimethoxyphenyl)ethene-1,1-diamine | KI | 96 nM | US-8772508: Inhibitors of glutaminyl cyclase |
| 2-(3H-benzimidazol-5-yl)-5-[2-(2-chloro-3-methoxyphenyl)ethyl]-1,3,4-thiadiazole | KI | 100 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| 6-[1-[2-(3,4-dimethoxyphenyl)ethyl]triazol-4-yl]-1H-benzimidazole | KI | 100 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| 6-[4-[(4-methoxyphenyl)methyl]-1,2,4-triazol-3-yl]-1H-benzimidazole | KI | 110 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| 6-[4-[(2,3-dichlorophenyl)methyl]-1,2,4-triazol-3-yl]-1H-benzimidazole | KI | 120 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| 2-(3H-benzimidazol-5-yl)-5-[2-(3-fluorophenyl)ethyl]-1,3,4-thiadiazole | KI | 120 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| 2-(3H-benzimidazol-5-yl)-5-(phenylsulfanylmethyl)-1,3,4-thiadiazole | KI | 120 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| 6-[1-(phenylsulfanylmethyl)triazol-4-yl]-1H-benzimidazole | KI | 120 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| 6-[1-[2-(3-methoxyphenyl)ethyl]triazol-4-yl]-1H-benzimidazole | KI | 120 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| 2-(3H-benzimidazol-5-yl)-5-[2-(3-chloro-4-methoxyphenyl)ethyl]-1,3,4-oxadiazole | KI | 130 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| 2-(3H-benzimidazol-5-yl)-5-[2-(2,4-difluorophenyl)ethyl]-1,3,4-thiadiazole | KI | 130 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| 2-(3H-benzimidazol-5-yl)-5-[2-(3,4-difluorophenyl)ethyl]-1,3,4-thiadiazole | KI | 140 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| 6-[1-(2-phenylethyl)triazol-4-yl]-1H-benzimidazole | KI | 140 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| 2-(3H-benzimidazol-5-yl)-5-[(3,4-dimethoxyphenyl)sulfonylmethyl]-1,3,4-thiadiazole | KI | 150 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| 2-(3H-benzimidazol-5-yl)-5-[2-(2-methoxyphenyl)ethyl]-1,3,4-thiadiazole | KI | 170 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| 2-(3H-benzimidazol-5-yl)-5-(2-phenylethyl)-1,3,4-thiadiazole | KI | 180 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| 6-[4-[(2-chlorophenyl)methyl]-1,2,4-triazol-3-yl]-1H-benzimidazole | KI | 200 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| 6-[4-[(3-chloro-4-methoxyphenyl)methyl]-1,2,4-triazol-3-yl]-1H-benzimidazole | KI | 230 nM | US-9181233: Inhibitors of glutaminyl cyclase |
| (E)-1-N-[3-(4-methylimidazol-1-yl)propyl]-1-N’-naphthalen-1-yl-2-nitroethene-1,1-diamine | IC50 | 7460 nM | US-8772508: Inhibitors of glutaminyl cyclase |
| (E)-1-N’-(4-chlorophenyl)-1-N-[3-(4-methylimidazol-1-yl)propyl]-2-nitroethene-1,1-diamine | IC50 | 8600 nM | US-8772508: Inhibitors of glutaminyl cyclase |
| (E)-1-N’-(3,4-dimethoxyphenyl)-1-N-[3-(4-methylimidazol-1-yl)propyl]-2-nitroethene-1,1-diamine | IC50 | 8730 nM | US-8772508: Inhibitors of glutaminyl cyclase |
ChEMBL bioactivities
172 potent at pChembl≥5 of 182 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
PubChem BioAssay actives
75 with measured affinity, of 94 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| 4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide | 2149165: Binding affinity to human QPCTL incubated for 45 mins by Kinobead based pull down assay | kd | 0.0058 | uM |
| (5S)-1-(3H-benzimidazol-5-yl)-5-(4-propoxyphenyl)imidazolidin-2-one | 2073000: Inhibition of gQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader | ic50 | 0.0100 | uM |
| 2-fluoro-5-[2-[4-(4-methyl-1,2,4-triazol-3-yl)piperidin-1-yl]-3-pyridinyl]pyridine | 2073000: Inhibition of gQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader | ic50 | 0.0130 | uM |
| 1-[4-[2-(2-amino-4-pyridinyl)ethoxy]-3-methoxyphenyl]-3-[3-(5-methylimidazol-1-yl)propyl]-1-(1-methylpiperidin-4-yl)urea | 1813087: Inhibition of isoQC (unknown origin) | ic50 | 0.0186 | uM |
| [4-[[3-[(E)-benzimidazol-5-ylidenemethyl]-2-hydroxy-1H-indol-4-yl]oxy]piperidin-1-yl]-thiophen-2-ylmethanone | 2073000: Inhibition of gQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader | ic50 | 0.0270 | uM |
| [4-[[3-[(E)-benzimidazol-5-ylidenemethyl]-2-hydroxy-1H-indol-4-yl]oxy]piperidin-1-yl]-(4-methoxyphenyl)methanone | 2073000: Inhibition of gQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader | ic50 | 0.0320 | uM |
| [4-[[3-[(E)-benzimidazol-5-ylidenemethyl]-2-hydroxy-1H-indol-4-yl]oxy]piperidin-1-yl]-pyridin-4-ylmethanone | 2073000: Inhibition of gQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader | ic50 | 0.0400 | uM |
| [4-[[3-[(E)-benzimidazol-5-ylidenemethyl]-2-hydroxy-1H-indol-4-yl]oxy]piperidin-1-yl]-phenylmethanone | 2073000: Inhibition of gQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader | ic50 | 0.0410 | uM |
| [4-[[3-[(E)-benzimidazol-5-ylidenemethyl]-2-hydroxy-1H-indol-4-yl]oxy]piperidin-1-yl]-(1-methylpyrazol-4-yl)methanone | 2073000: Inhibition of gQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader | ic50 | 0.0450 | uM |
| [4-[[3-[(E)-benzimidazol-5-ylidenemethyl]-2-hydroxy-1H-indol-4-yl]oxy]piperidin-1-yl]-(oxan-4-yl)methanone | 2073000: Inhibition of gQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader | ic50 | 0.0560 | uM |
| 2-(3H-benzimidazol-5-yl)-5-[(3,4-dimethoxyphenyl)sulfanylmethyl]-1,3,4-thiadiazole | 2073000: Inhibition of gQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader | ic50 | 0.0700 | uM |
| 5-[1-[[3-methoxy-4-(3-morpholin-4-ylpropoxy)phenyl]methyl]benzimidazol-5-yl]-1,3,4-thiadiazol-2-amine | 1893770: Inhibition of recombinant human isoQC using H-Gln-AMC hydrobromide as fluorogenic substrate incubated for 6 hrs by fluorometric microplate reader analysis | ic50 | 0.0720 | uM |
| 5-[1-[[3-methoxy-4-(3-piperidin-1-ylpropoxy)phenyl]methyl]benzimidazol-5-yl]-1,3,4-thiadiazol-2-amine | 1893770: Inhibition of recombinant human isoQC using H-Gln-AMC hydrobromide as fluorogenic substrate incubated for 6 hrs by fluorometric microplate reader analysis | ic50 | 0.0730 | uM |
| 1-[(4-fluorophenyl)methyl]-3-[3-(5-methylimidazol-1-yl)propyl]-1-(3-methyl-2H-indazol-6-yl)urea | 1945964: Inhibition of isoQC (unknown origin) | ic50 | 0.0796 | uM |
| 1-(cyclopentylmethyl)-3-[3-(5-methylimidazol-1-yl)propyl]-1-(3-methyl-2H-indazol-6-yl)urea | 1945964: Inhibition of isoQC (unknown origin) | ic50 | 0.0879 | uM |
| 5-[1-[(4-fluorophenyl)methyl]benzimidazol-5-yl]-1,3,4-thiadiazol-2-amine | 1893770: Inhibition of recombinant human isoQC using H-Gln-AMC hydrobromide as fluorogenic substrate incubated for 6 hrs by fluorometric microplate reader analysis | ic50 | 0.1040 | uM |
| 1-cyclohexyl-3-[3-(5-methylimidazol-1-yl)propyl]-1-(3-methyl-2H-indazol-6-yl)urea | 1945964: Inhibition of isoQC (unknown origin) | ic50 | 0.1061 | uM |
| 1-[4-[[3-[(E)-benzimidazol-5-ylidenemethyl]-2-hydroxy-1H-indol-4-yl]oxy]piperidin-1-yl]ethanone | 2073000: Inhibition of gQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader | ic50 | 0.1300 | uM |
| 1-[4-[[3-[(E)-benzimidazol-5-ylidenemethyl]-2-hydroxy-1H-indol-4-yl]oxy]piperidin-1-yl]-3-methoxypropan-1-one | 2073000: Inhibition of gQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader | ic50 | 0.1400 | uM |
| 5-[1-(1,3-benzodioxol-5-ylmethyl)benzimidazol-5-yl]-1,3,4-thiadiazol-2-amine | 1893770: Inhibition of recombinant human isoQC using H-Gln-AMC hydrobromide as fluorogenic substrate incubated for 6 hrs by fluorometric microplate reader analysis | ic50 | 0.1520 | uM |
| 3-[[5-(5-amino-1,3,4-thiadiazol-2-yl)benzimidazol-1-yl]methyl]benzonitrile | 1893770: Inhibition of recombinant human isoQC using H-Gln-AMC hydrobromide as fluorogenic substrate incubated for 6 hrs by fluorometric microplate reader analysis | ic50 | 0.1570 | uM |
| 5-[1-[(3,4-difluorophenyl)methyl]benzimidazol-5-yl]-1,3,4-thiadiazol-2-amine | 1893770: Inhibition of recombinant human isoQC using H-Gln-AMC hydrobromide as fluorogenic substrate incubated for 6 hrs by fluorometric microplate reader analysis | ic50 | 0.1720 | uM |
| 5-[1-[(3,4-dimethoxyphenyl)methyl]benzimidazol-5-yl]-1,3,4-thiadiazol-2-amine | 1893770: Inhibition of recombinant human isoQC using H-Gln-AMC hydrobromide as fluorogenic substrate incubated for 6 hrs by fluorometric microplate reader analysis | ic50 | 0.1730 | uM |
| [4-[[3-[(E)-benzimidazol-5-ylidenemethyl]-2-hydroxy-1H-indol-4-yl]oxy]piperidin-1-yl]-cyclopropylmethanone | 2073000: Inhibition of gQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader | ic50 | 0.1800 | uM |
| 5-[1-[[3-methoxy-4-(3-pyridin-2-ylpropoxy)phenyl]methyl]benzimidazol-5-yl]-1,3,4-thiadiazol-2-amine | 1893770: Inhibition of recombinant human isoQC using H-Gln-AMC hydrobromide as fluorogenic substrate incubated for 6 hrs by fluorometric microplate reader analysis | ic50 | 0.2020 | uM |
| 1-[4-[4-(2-amino-4-pyridinyl)butoxy]-3-methoxyphenyl]-3-(3H-benzimidazol-5-ylmethyl)-1-(1-methylpiperidin-4-yl)urea | 1813087: Inhibition of isoQC (unknown origin) | ic50 | 0.2130 | uM |
| 5-[1-[(3,4-dimethylphenyl)methyl]benzimidazol-5-yl]-1,3,4-thiadiazol-2-amine | 1893770: Inhibition of recombinant human isoQC using H-Gln-AMC hydrobromide as fluorogenic substrate incubated for 6 hrs by fluorometric microplate reader analysis | ic50 | 0.2190 | uM |
| 5-[1-[(3-methoxyphenyl)methyl]benzimidazol-5-yl]-1,3,4-thiadiazol-2-amine | 1893770: Inhibition of recombinant human isoQC using H-Gln-AMC hydrobromide as fluorogenic substrate incubated for 6 hrs by fluorometric microplate reader analysis | ic50 | 0.2390 | uM |
| [4-[[3-[(E)-benzimidazol-5-ylidenemethyl]-2-hydroxy-1H-indol-4-yl]oxy]piperidin-1-yl]-(3,4-dimethoxyphenyl)methanone | 2073000: Inhibition of gQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader | ic50 | 0.2900 | uM |
| 5-[1-[(4-chloro-3-fluorophenyl)methyl]benzimidazol-5-yl]-1,3,4-thiadiazol-2-amine | 1893770: Inhibition of recombinant human isoQC using H-Gln-AMC hydrobromide as fluorogenic substrate incubated for 6 hrs by fluorometric microplate reader analysis | ic50 | 0.2970 | uM |
| 5-(3H-benzimidazol-5-yl)-1,2-dihydro-1,2,4-triazole-3-thione | 1893770: Inhibition of recombinant human isoQC using H-Gln-AMC hydrobromide as fluorogenic substrate incubated for 6 hrs by fluorometric microplate reader analysis | ic50 | 0.2980 | uM |
| 1-(3,4-dimethoxyphenyl)-3-[3-(5-methylimidazol-1-yl)propyl]-1-(1-methylpiperidin-4-yl)urea | 1577857: Inhibition of isoQC (unknown origin) | ic50 | 0.3040 | uM |
| N-[4-(2-amino-1,3-thiazol-5-yl)phenyl]-3,4-dimethoxybenzenesulfonamide | 2073043: Binding affinity to gQC (unknown origin) assessed as inhibition constant at pH 8 | ki | 0.3400 | uM |
| 5-[1-[(4-methoxyphenyl)methyl]benzimidazol-5-yl]-1,3,4-thiadiazol-2-amine | 1893770: Inhibition of recombinant human isoQC using H-Gln-AMC hydrobromide as fluorogenic substrate incubated for 6 hrs by fluorometric microplate reader analysis | ic50 | 0.3420 | uM |
| 3-[(E)-benzimidazol-5-ylidenemethyl]-4-(1-methylsulfonylpiperidin-4-yl)oxy-1H-indol-2-ol | 2073000: Inhibition of gQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader | ic50 | 0.3500 | uM |
| 1-(3,4-dimethoxyphenyl)-3-(3-imidazol-1-ylpropyl)thiourea | 1893770: Inhibition of recombinant human isoQC using H-Gln-AMC hydrobromide as fluorogenic substrate incubated for 6 hrs by fluorometric microplate reader analysis | ic50 | 0.3510 | uM |
| 5-(3H-benzimidazol-5-yl)-1,3,4-thiadiazol-2-amine | 1893770: Inhibition of recombinant human isoQC using H-Gln-AMC hydrobromide as fluorogenic substrate incubated for 6 hrs by fluorometric microplate reader analysis | ic50 | 0.3530 | uM |
| 5-[1-[[4-(trifluoromethyl)phenyl]methyl]benzimidazol-5-yl]-1,3,4-thiadiazol-2-amine | 1893770: Inhibition of recombinant human isoQC using H-Gln-AMC hydrobromide as fluorogenic substrate incubated for 6 hrs by fluorometric microplate reader analysis | ic50 | 0.3590 | uM |
| 3-[(E)-benzimidazol-5-ylidenemethyl]-4-(oxan-3-yloxy)-1H-indol-2-ol | 2073000: Inhibition of gQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader | ic50 | 0.4100 | uM |
| 3-[(E)-benzimidazol-5-ylidenemethyl]-4-(4-hydroxycyclohexyl)oxy-1H-indol-2-ol | 2073000: Inhibition of gQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader | ic50 | 0.4100 | uM |
| 6-[3-[(3-methoxyphenyl)methylsulfanyl]-1H-1,2,4-triazol-5-yl]-1H-benzimidazole | 1893770: Inhibition of recombinant human isoQC using H-Gln-AMC hydrobromide as fluorogenic substrate incubated for 6 hrs by fluorometric microplate reader analysis | ic50 | 0.4140 | uM |
| 1-[4-[4-(6-amino-3-pyridinyl)butoxy]-3-methoxyphenyl]-3-[3-(5-methylimidazol-1-yl)propyl]thiourea | 2073000: Inhibition of gQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader | ic50 | 0.5020 | uM |
| 1-[4-[4-(2-amino-4-pyridinyl)butoxy]-3-methoxyphenyl]-3-[3-(5-methylimidazol-1-yl)propyl]thiourea | 1442140: Inhibition of iso glutaminyl cyclase (unknown origin) | ic50 | 0.5020 | uM |
| 5-(1H-indazol-5-yl)-1,3,4-thiadiazol-2-amine | 1893770: Inhibition of recombinant human isoQC using H-Gln-AMC hydrobromide as fluorogenic substrate incubated for 6 hrs by fluorometric microplate reader analysis | ic50 | 0.5140 | uM |
| 3-[(E)-benzimidazol-5-ylidenemethyl]-4-(oxan-4-yloxy)-1H-indol-2-ol | 2073000: Inhibition of gQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader | ic50 | 0.5700 | uM |
| 3-[(E)-benzimidazol-5-ylidenemethyl]-4-bromo-1H-indol-2-ol | 2073000: Inhibition of gQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader | ic50 | 0.6600 | uM |
| N-[3-[(E)-benzimidazol-5-ylidenemethyl]-2-hydroxy-1H-indol-4-yl]-3,4-dimethoxybenzamide | 2073000: Inhibition of gQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader | ic50 | 0.8900 | uM |
| 3-[(E)-benzimidazol-5-ylidenemethyl]-4-(oxolan-3-yloxy)-1H-indol-2-ol | 2073000: Inhibition of gQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader | ic50 | 0.9000 | uM |
| 3-[(E)-benzimidazol-5-ylidenemethyl]-4-(4-methoxycyclohexyl)oxy-1H-indol-2-ol | 2073000: Inhibition of gQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader | ic50 | 0.9000 | uM |
| 3-[(E)-benzimidazol-5-ylidenemethyl]-4-bromo-1-methylindol-2-ol | 2073000: Inhibition of gQC (unknown origin) expressed in Escherichia coli Transetta (DE3) assessed as N-terminal pyroglutamate formation using fluorescent substrate H-Gln-AMC incubated for 12 hrs by microplate reader | ic50 | 0.9400 | uM |
CTD chemical–gene interactions
13 total (human), top 13 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| triphenyl phosphate | affects expression | 1 |
| pirinixic acid | increases activity, affects binding, decreases expression | 1 |
| sodium arsenate | increases expression | 1 |
| di-n-butylphosphoric acid | affects expression | 1 |
| 2-palmitoylglycerol | increases expression | 1 |
| abrine | decreases expression | 1 |
| jinfukang | increases expression | 1 |
| Resveratrol | affects cotreatment, decreases expression | 1 |
| Sunitinib | increases expression | 1 |
| Diazinon | increases methylation | 1 |
| Doxorubicin | decreases expression | 1 |
| Plant Extracts | affects cotreatment, decreases expression | 1 |
| Smoke | decreases expression | 1 |
ChEMBL screening assays
16 unique, capped per target: 16 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL3706344 | Binding | Fluorometric Assay: All measurements were performed with a BioAssay Reader HTS-7000Plus for microplates (Perkin Elmer) at 30C. QC activity was evaluated fluorometrically using H-Gln-beta NA. The samples consisted of 0.2 mM fluorogenic subst | Inhibitors of glutaminyl cyclase |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.