Assay Detail
Binding
CHEMBL1166367
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Inhibition of Bacillus thermoproteolyticus thermolysin after 15 mins by microplate fluorescence analysis in presence of 0.5 to 2 mM substrate FaGLa
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bacillus thermoproteolyticus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Identification of novel quinazolin-4(3H)-ones as inhibitors of thermolysin, the prototype of the M4 family of proteinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 5.39 | 7.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1164452 | — | — | 1 | 7.94 |
| CHEMBL1163762 | — | — | 1 | 6.61 |
| CHEMBL1163173 | — | — | 1 | 5.90 |
| CHEMBL1163157 | — | — | 1 | 4.42 |
| CHEMBL1163745 | — | — | 1 | 4.38 |
| CHEMBL1163152 | — | — | 1 | 4.26 |
| CHEMBL1164862 | — | — | 1 | 4.23 |
| CHEMBL1164980 | — | — | 1 | - |
| CHEMBL1164655 | — | — | 1 | - |
| CHEMBL1164450 | — | — | 1 | - |
| CHEMBL1163632 | — | — | 1 | - |
| CHEMBL1163684 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1164452 | — | Ki | = | 11.5 | nM | 7.94 |
| CHEMBL1163762 | — | Ki | = | 243.0 | nM | 6.61 |
| CHEMBL1163173 | — | Ki | = | 1250.0 | nM | 5.90 |
| CHEMBL1163157 | — | Ki | = | 37900.0 | nM | 4.42 |
| CHEMBL1163745 | — | Ki | = | 42000.0 | nM | 4.38 |
| CHEMBL1163152 | — | Ki | = | 54900.0 | nM | 4.26 |
| CHEMBL1164862 | — | Ki | = | 59300.0 | nM | 4.23 |
| CHEMBL1164980 | — | Ki | = | 3120000.0 | nM | - |
| CHEMBL1164655 | — | Ki | = | 10100000.0 | nM | - |
| CHEMBL1164450 | — | Ki | = | 1830000.0 | nM | - |
| CHEMBL1163632 | — | Ki | = | 4000000.0 | nM | - |
| CHEMBL1163684 | — | Ki | = | 106000000.0 | nM | - |