Assay Detail
Binding
CHEMBL697873
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In vitro inhibition of human tryptase.
21
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 8.15 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL322526 | — | — | 1 | 9.40 |
| CHEMBL322538 | — | — | 1 | 9.15 |
| CHEMBL110061 | — | — | 1 | 9.15 |
| CHEMBL109888 | — | — | 1 | 9.00 |
| CHEMBL443539 | — | — | 1 | 9.00 |
| CHEMBL111250 | — | — | 1 | 9.00 |
| CHEMBL107493 | — | — | 1 | 8.52 |
| CHEMBL71037 | — | — | 1 | 8.40 |
| CHEMBL321622 | — | — | 1 | 8.40 |
| CHEMBL109947 | — | — | 1 | 8.30 |
| CHEMBL111548 | — | — | 1 | 8.28 |
| CHEMBL320744 | — | — | 3 | 8.22 |
| CHEMBL326480 | — | — | 1 | 8.15 |
| CHEMBL111270 | — | — | 1 | 8.05 |
| CHEMBL109254 | — | — | 1 | 8.05 |
| CHEMBL109882 | — | — | 1 | 7.96 |
| CHEMBL109602 | — | — | 1 | 7.89 |
| CHEMBL111141 | — | — | 1 | 7.75 |
| CHEMBL320529 | — | — | 1 | 7.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL322526 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL322538 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL110061 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL109888 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL443539 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL111250 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL107493 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL71037 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL321622 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL109947 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL111548 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL320744 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL326480 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL111270 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL109254 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL109882 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL109602 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL111141 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL320529 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL320744 | — | IC50 | = | 992.0 | nM | 6.00 |
| CHEMBL320744 | — | IC50 | = | 5380.0 | nM | 5.27 |