Assay Detail
Binding
CHEMBL4376103
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal His6-tagged glutaminyl cyclase (Ala33 to Leu361 residues) expressed in baculovirus infected Sf21 insect cells using H-Gln-AMC hydrobromide as substrate measured in presence of pGAPase by fluorometric assay
68
Total Activities
68
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Conformationally Restricted Human Glutaminyl Cyclase Inhibitors as Potent Anti-Alzheimer's Agents by Structure-Based Design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 68 | 7.78 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4525926 | — | — | 1 | 8.89 |
| CHEMBL4445407 | — | — | 1 | 8.80 |
| CHEMBL4464130 | — | — | 1 | 8.55 |
| CHEMBL4539841 | — | — | 1 | 8.47 |
| CHEMBL4586501 | — | — | 1 | 8.46 |
| CHEMBL4547037 | — | — | 1 | 8.44 |
| CHEMBL4448303 | — | — | 1 | 8.41 |
| CHEMBL4445143 | — | — | 1 | 8.39 |
| CHEMBL4549443 | — | — | 1 | 8.35 |
| CHEMBL4097599 | — | — | 1 | 8.35 |
| CHEMBL4459792 | — | — | 1 | 8.34 |
| CHEMBL4462968 | — | — | 1 | 8.33 |
| CHEMBL4590359 | — | — | 1 | 8.28 |
| CHEMBL4472311 | — | — | 1 | 8.27 |
| CHEMBL4459555 | — | — | 1 | 8.25 |
| CHEMBL4589039 | — | — | 1 | 8.21 |
| CHEMBL4446821 | — | — | 1 | 8.21 |
| CHEMBL4582369 | — | — | 1 | 8.19 |
| CHEMBL4520303 | — | — | 1 | 8.17 |
| CHEMBL4448862 | — | — | 1 | 8.12 |
| CHEMBL4578714 | — | — | 1 | 8.12 |
| CHEMBL4471709 | — | — | 1 | 8.09 |
| CHEMBL4434757 | — | — | 1 | 8.07 |
| CHEMBL4440547 | — | — | 1 | 8.06 |
| CHEMBL4567619 | — | — | 1 | 8.06 |
| CHEMBL4464265 | — | — | 1 | 7.96 |
| CHEMBL4586829 | — | — | 1 | 7.91 |
| CHEMBL4520053 | — | — | 1 | 7.90 |
| CHEMBL4475906 | — | — | 1 | 7.89 |
| CHEMBL4452351 | — | — | 1 | 7.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4525926 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4445407 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4464130 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4539841 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4586501 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4547037 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4448303 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4445143 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4549443 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4097599 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4459792 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4462968 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL4590359 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL4472311 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4459555 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4589039 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4446821 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL4582369 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4520303 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL4448862 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL4578714 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL4471709 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL4434757 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL4440547 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL4567619 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL4464265 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4586829 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL4520053 | — | IC50 | = | 12.5 | nM | 7.90 |
| CHEMBL4475906 | — | IC50 | = | 12.9 | nM | 7.89 |
| CHEMBL4452351 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL4579239 | — | IC50 | = | 13.6 | nM | 7.87 |
| CHEMBL4539950 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4443747 | — | IC50 | = | 16.4 | nM | 7.79 |
| CHEMBL4462495 | — | IC50 | = | 16.7 | nM | 7.78 |
| CHEMBL4469263 | — | IC50 | = | 17.5 | nM | 7.76 |
| CHEMBL4436441 | — | IC50 | = | 17.6 | nM | 7.75 |
| CHEMBL4451831 | — | IC50 | = | 19.4 | nM | 7.71 |
| CHEMBL4585964 | — | IC50 | = | 20.5 | nM | 7.69 |
| CHEMBL4454399 | — | IC50 | = | 22.9 | nM | 7.64 |
| CHEMBL4474239 | — | IC50 | = | 23.5 | nM | 7.63 |
| CHEMBL4438809 | — | IC50 | = | 23.3 | nM | 7.63 |
| CHEMBL4470465 | — | IC50 | = | 24.3 | nM | 7.61 |
| CHEMBL4589697 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4578087 | — | IC50 | = | 25.6 | nM | 7.59 |
| CHEMBL4586610 | — | IC50 | = | 26.5 | nM | 7.58 |
| CHEMBL4476133 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3659476 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL566563 | — | IC50 | = | 29.2 | nM | 7.54 |
| CHEMBL4445955 | — | IC50 | = | 30.6 | nM | 7.51 |
| CHEMBL4469107 | — | IC50 | = | 32.5 | nM | 7.49 |