Assay Detail
Binding
CHEMBL4009736
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Inhibition of human glutaminyl cyclase assessed as reduction in conversion of H-Gln-AMC hydrobromide to pGlu-AMC preincubated with substrate for 10 mins followed by enzyme addition by pGAPase coupled fluorometry
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Potent Human Glutaminyl Cyclase Inhibitors as Anti-Alzheimer's Agents Based on Rational Design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 53 | 7.89 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4077433 | — | — | 1 | 9.15 |
| CHEMBL4070663 | — | — | 1 | 8.43 |
| CHEMBL4097599 | — | — | 1 | 8.35 |
| CHEMBL4093071 | — | — | 1 | 8.34 |
| CHEMBL4099813 | — | — | 1 | 8.32 |
| CHEMBL4082916 | — | — | 1 | 8.28 |
| CHEMBL4074799 | — | — | 1 | 8.26 |
| CHEMBL4075925 | — | — | 1 | 8.24 |
| CHEMBL4088456 | — | — | 1 | 8.16 |
| CHEMBL4071297 | — | — | 1 | 8.14 |
| CHEMBL4073599 | — | — | 1 | 8.14 |
| CHEMBL4099260 | — | — | 1 | 8.11 |
| CHEMBL4082802 | — | — | 1 | 8.11 |
| CHEMBL4062645 | — | — | 1 | 8.09 |
| CHEMBL4084521 | — | — | 1 | 8.08 |
| CHEMBL4062842 | — | — | 1 | 8.05 |
| CHEMBL4093243 | — | — | 1 | 8.04 |
| CHEMBL4100758 | — | — | 1 | 8.04 |
| CHEMBL4074222 | — | — | 1 | 7.97 |
| CHEMBL4081803 | — | — | 1 | 7.94 |
| CHEMBL4098332 | — | — | 1 | 7.93 |
| CHEMBL4102431 | — | — | 1 | 7.91 |
| CHEMBL4062616 | — | — | 1 | 7.90 |
| CHEMBL4090828 | — | — | 1 | 7.90 |
| CHEMBL4097231 | — | — | 1 | 7.89 |
| CHEMBL4063751 | — | — | 1 | 7.87 |
| CHEMBL4100893 | — | — | 1 | 7.86 |
| CHEMBL4090608 | — | — | 1 | 7.86 |
| CHEMBL4085595 | — | — | 1 | 7.85 |
| CHEMBL4063693 | — | — | 1 | 7.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4077433 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4070663 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4097599 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4093071 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4099813 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4082916 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4074799 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL4075925 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL4088456 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL4071297 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL4073599 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4099260 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL4082802 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4062645 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL4084521 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL4062842 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4093243 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL4100758 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL4074222 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL4081803 | — | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL4098332 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL4102431 | — | IC50 | = | 12.3 | nM | 7.91 |
| CHEMBL4062616 | — | IC50 | = | 12.5 | nM | 7.90 |
| CHEMBL4090828 | — | IC50 | = | 12.5 | nM | 7.90 |
| CHEMBL4097231 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4063751 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL4090608 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL4100893 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL4085595 | — | IC50 | = | 14.1 | nM | 7.85 |
| CHEMBL4063693 | — | IC50 | = | 14.4 | nM | 7.84 |
| CHEMBL4093854 | — | IC50 | = | 15.3 | nM | 7.82 |
| CHEMBL4089521 | — | IC50 | = | 16.2 | nM | 7.79 |
| CHEMBL4066278 | — | IC50 | = | 16.6 | nM | 7.78 |
| CHEMBL4059704 | — | IC50 | = | 17.5 | nM | 7.76 |
| CHEMBL4076559 | — | IC50 | = | 17.5 | nM | 7.76 |
| CHEMBL4092890 | — | IC50 | = | 18.4 | nM | 7.74 |
| CHEMBL4086721 | — | IC50 | = | 18.5 | nM | 7.73 |
| CHEMBL4070421 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4074894 | — | IC50 | = | 19.3 | nM | 7.71 |
| CHEMBL4077135 | — | IC50 | = | 20.2 | nM | 7.70 |
| CHEMBL4065599 | — | IC50 | = | 19.8 | nM | 7.70 |
| CHEMBL4063517 | — | IC50 | = | 20.5 | nM | 7.69 |
| CHEMBL4075609 | — | IC50 | = | 21.3 | nM | 7.67 |
| CHEMBL4076975 | — | IC50 | = | 23.5 | nM | 7.63 |
| CHEMBL4065376 | — | IC50 | = | 24.7 | nM | 7.61 |
| CHEMBL566563 | — | IC50 | = | 29.2 | nM | 7.54 |
| CHEMBL4093175 | — | IC50 | = | 30.2 | nM | 7.52 |
| CHEMBL4101582 | — | IC50 | = | 35.5 | nM | 7.45 |
| CHEMBL4081649 | — | IC50 | = | 39.4 | nM | 7.41 |
| CHEMBL4061029 | — | IC50 | = | 38.7 | nM | 7.41 |