Assay Detail
Binding
CHEMBL3706344
Review assay metadata, readout intent, target linkage, and publication context from the same page.
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 substrate, 0.25 U pyroglutamyl aminopeptidase (Unizyme, Horsholm, Denmark) in 0.2 M Tris/HCl, pH 8.0 containing 20 mM EDTA and an appropriately diluted aliquot of QC in a final volume of 250 ul. Excitation/emission wavelengths were 320/410 nm. The assay reactions were initiated by addition of glutaminyl cyclase. QC activity was determined from a standard curve of beta -naphthylamine under assay conditions. One unit is defined as the amount of QC catalyzing the formation of 1 umol pGlu-beta NA from H-Gln-beta NA per minute under the described conditions. In a second fluorometric assay, QC was activity determined using H-Gln-AMC as substrate. Reactions were carried out at 30C. utilizing the NOVOStar reader for microplates (BMG labtechnologies).
27
Total Activities
17
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Glutaminyl-peptide cyclotransferase-like protein (CHEMBL3638349) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Inhibitors of glutaminyl cyclase
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.82 | 6.64 |
| Ki | 10 | 7.30 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3649507 | — | — | 2 | 7.96 |
| CHEMBL3649517 | — | — | 2 | 7.47 |
| CHEMBL3649518 | — | — | 2 | 7.39 |
| CHEMBL3649516 | — | — | 2 | 7.29 |
| CHEMBL3649504 | — | — | 2 | 7.26 |
| CHEMBL3649508 | — | — | 2 | 7.17 |
| CHEMBL3649519 | — | — | 2 | 7.17 |
| CHEMBL3649506 | — | — | 2 | 7.12 |
| CHEMBL3649515 | — | — | 2 | 7.10 |
| CHEMBL3649505 | — | — | 2 | 7.02 |
| CHEMBL3649513 | — | — | 1 | 5.13 |
| CHEMBL3649509 | — | — | 1 | 5.07 |
| CHEMBL3649514 | — | — | 1 | 5.06 |
| CHEMBL3649510 | — | — | 1 | 5.06 |
| CHEMBL3649511 | — | — | 1 | 5.03 |
| CHEMBL3639483 | — | — | 1 | 5.01 |
| CHEMBL3649512 | — | — | 1 | 4.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3649507 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL3649517 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL3649518 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL3649516 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL3649504 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL3649519 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL3649508 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL3649506 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL3649515 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL3649505 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL3649518 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3649516 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL3649508 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3649515 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3649517 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL3649519 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL3649504 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL3649507 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL3649505 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL3649506 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL3649513 | — | IC50 | = | 7460.0 | nM | 5.13 |
| CHEMBL3649509 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL3649514 | — | IC50 | = | 8790.0 | nM | 5.06 |
| CHEMBL3649510 | — | IC50 | = | 8730.0 | nM | 5.06 |
| CHEMBL3649511 | — | IC50 | = | 9450.0 | nM | 5.03 |
| CHEMBL3639483 | — | IC50 | = | 9680.0 | nM | 5.01 |
| CHEMBL3649512 | — | IC50 | = | 10400.0 | nM | 4.98 |