Assay Detail
Binding
CHEMBL660458
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In vitro inhibitory activity was determined against bovine pancreas chymotrypsin
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis, structure-activity relationships, and pharmacokinetic profiles of nonpeptidic difluoromethylene ketones as novel inhibitors of human chymase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 6.16 | 8.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL247767 | CHYMOSTATIN | — | 1 | 8.03 |
| CHEMBL26494 | — | — | 1 | 7.90 |
| CHEMBL283786 | — | — | 1 | 6.96 |
| CHEMBL26182 | — | — | 1 | 6.83 |
| CHEMBL23910 | — | — | 1 | 6.77 |
| CHEMBL284017 | — | — | 1 | 6.75 |
| CHEMBL275228 | — | — | 1 | 6.62 |
| CHEMBL284138 | — | — | 1 | 6.55 |
| CHEMBL26333 | — | — | 1 | 6.53 |
| CHEMBL284005 | — | — | 1 | 6.51 |
| CHEMBL26496 | — | — | 1 | 6.46 |
| CHEMBL287318 | — | — | 1 | 6.44 |
| CHEMBL24697 | — | — | 1 | 6.35 |
| CHEMBL24734 | — | — | 1 | 6.34 |
| CHEMBL280377 | — | — | 1 | 6.34 |
| CHEMBL284702 | — | — | 1 | 6.11 |
| CHEMBL284495 | — | — | 1 | 5.96 |
| CHEMBL25199 | — | — | 1 | 5.85 |
| CHEMBL25169 | — | — | 1 | 5.84 |
| CHEMBL24071 | — | — | 1 | 5.84 |
| CHEMBL442146 | — | — | 1 | 5.74 |
| CHEMBL25833 | — | — | 1 | 5.72 |
| CHEMBL25884 | — | — | 1 | 5.71 |
| CHEMBL26448 | — | — | 1 | 5.49 |
| CHEMBL24670 | — | — | 1 | 5.48 |
| CHEMBL24707 | — | — | 1 | 5.45 |
| CHEMBL24211 | — | — | 1 | 4.86 |
| CHEMBL25114 | — | — | 1 | 4.75 |
| CHEMBL418568 | — | — | 1 | 4.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL247767 | CHYMOSTATIN | Ki | = | 9.36 | nM | 8.03 |
| CHEMBL26494 | — | Ki | = | 12.6 | nM | 7.90 |
| CHEMBL283786 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL26182 | — | Ki | = | 147.0 | nM | 6.83 |
| CHEMBL23910 | — | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL284017 | — | Ki | = | 177.0 | nM | 6.75 |
| CHEMBL275228 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL284138 | — | Ki | = | 282.0 | nM | 6.55 |
| CHEMBL26333 | — | Ki | = | 295.0 | nM | 6.53 |
| CHEMBL284005 | — | Ki | = | 306.0 | nM | 6.51 |
| CHEMBL26496 | — | Ki | = | 348.0 | nM | 6.46 |
| CHEMBL287318 | — | Ki | = | 364.0 | nM | 6.44 |
| CHEMBL24697 | — | Ki | = | 451.0 | nM | 6.35 |
| CHEMBL24734 | — | Ki | = | 458.0 | nM | 6.34 |
| CHEMBL280377 | — | Ki | = | 455.0 | nM | 6.34 |
| CHEMBL284702 | — | Ki | = | 780.0 | nM | 6.11 |
| CHEMBL284495 | — | Ki | = | 1090.0 | nM | 5.96 |
| CHEMBL25199 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL25169 | — | Ki | = | 1440.0 | nM | 5.84 |
| CHEMBL24071 | — | Ki | = | 1430.0 | nM | 5.84 |
| CHEMBL442146 | — | Ki | = | 1830.0 | nM | 5.74 |
| CHEMBL25833 | — | Ki | = | 1920.0 | nM | 5.72 |
| CHEMBL25884 | — | Ki | = | 1960.0 | nM | 5.71 |
| CHEMBL26448 | — | Ki | = | 3220.0 | nM | 5.49 |
| CHEMBL24670 | — | Ki | = | 3280.0 | nM | 5.48 |
| CHEMBL24707 | — | Ki | = | 3570.0 | nM | 5.45 |
| CHEMBL24211 | — | Ki | = | 13700.0 | nM | 4.86 |
| CHEMBL25114 | — | Ki | = | 17900.0 | nM | 4.75 |
| CHEMBL418568 | — | Ki | = | 27800.0 | nM | 4.56 |