Assay Detail
Binding
CHEMBL807472
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory activity was determined against human heart chymase
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 | 7.67 | 8.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL24734 | — | — | 1 | 8.58 |
| CHEMBL26448 | — | — | 1 | 8.45 |
| CHEMBL287318 | — | — | 1 | 8.25 |
| CHEMBL25199 | — | — | 1 | 8.11 |
| CHEMBL25884 | — | — | 1 | 8.03 |
| CHEMBL284702 | — | — | 1 | 8.01 |
| CHEMBL26182 | — | — | 1 | 7.99 |
| CHEMBL24707 | — | — | 1 | 7.99 |
| CHEMBL25169 | — | — | 1 | 7.92 |
| CHEMBL247767 | CHYMOSTATIN | — | 1 | 7.88 |
| CHEMBL26494 | — | — | 1 | 7.88 |
| CHEMBL283786 | — | — | 1 | 7.86 |
| CHEMBL284005 | — | — | 1 | 7.80 |
| CHEMBL284138 | — | — | 1 | 7.78 |
| CHEMBL442146 | — | — | 1 | 7.77 |
| CHEMBL25833 | — | — | 1 | 7.77 |
| CHEMBL24697 | — | — | 1 | 7.73 |
| CHEMBL24071 | — | — | 1 | 7.64 |
| CHEMBL284495 | — | — | 1 | 7.54 |
| CHEMBL284017 | — | — | 1 | 7.49 |
| CHEMBL26333 | — | — | 1 | 7.47 |
| CHEMBL280377 | — | — | 1 | 7.30 |
| CHEMBL23910 | — | — | 1 | 7.13 |
| CHEMBL275228 | — | — | 1 | 7.07 |
| CHEMBL26496 | — | — | 1 | 7.04 |
| CHEMBL24670 | — | — | 1 | 6.36 |
| CHEMBL24211 | — | — | 1 | 6.31 |
| CHEMBL25114 | — | — | 1 | - |
| CHEMBL418568 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL24734 | — | Ki | = | 2.62 | nM | 8.58 |
| CHEMBL26448 | — | Ki | = | 3.56 | nM | 8.45 |
| CHEMBL287318 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL25199 | — | Ki | = | 7.71 | nM | 8.11 |
| CHEMBL25884 | — | Ki | = | 9.32 | nM | 8.03 |
| CHEMBL284702 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL26182 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL24707 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL25169 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL247767 | CHYMOSTATIN | Ki | = | 13.1 | nM | 7.88 |
| CHEMBL26494 | — | Ki | = | 13.3 | nM | 7.88 |
| CHEMBL283786 | — | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL284005 | — | Ki | = | 15.7 | nM | 7.80 |
| CHEMBL284138 | — | Ki | = | 16.6 | nM | 7.78 |
| CHEMBL442146 | — | Ki | = | 16.9 | nM | 7.77 |
| CHEMBL25833 | — | Ki | = | 16.9 | nM | 7.77 |
| CHEMBL24697 | — | Ki | = | 18.5 | nM | 7.73 |
| CHEMBL24071 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL284495 | — | Ki | = | 28.9 | nM | 7.54 |
| CHEMBL284017 | — | Ki | = | 32.5 | nM | 7.49 |
| CHEMBL26333 | — | Ki | = | 33.7 | nM | 7.47 |
| CHEMBL280377 | — | Ki | = | 50.6 | nM | 7.30 |
| CHEMBL23910 | — | Ki | = | 74.3 | nM | 7.13 |
| CHEMBL275228 | — | Ki | = | 84.7 | nM | 7.07 |
| CHEMBL26496 | — | Ki | = | 90.7 | nM | 7.04 |
| CHEMBL24670 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL24211 | — | Ki | = | 489.0 | nM | 6.31 |
| CHEMBL25114 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL418568 | — | Ki | > | 10000.0 | nM | - |