Assay Detail
Binding
CHEMBL815470
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Inhibitory constant against human trypsin
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 5.26 | 6.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL143418 | — | — | 1 | 6.10 |
| CHEMBL143139 | — | — | 1 | 6.10 |
| CHEMBL142546 | — | — | 1 | 6.07 |
| CHEMBL142566 | — | — | 1 | 5.80 |
| CHEMBL19080 | L-375378 | — | 1 | 5.75 |
| CHEMBL143138 | — | — | 1 | 5.44 |
| CHEMBL143008 | — | — | 1 | 5.42 |
| CHEMBL143421 | — | — | 1 | 5.34 |
| CHEMBL341909 | — | — | 1 | 4.40 |
| CHEMBL356296 | — | — | 1 | 4.33 |
| CHEMBL422299 | — | — | 1 | 4.21 |
| CHEMBL142240 | — | — | 1 | 4.10 |
| CHEMBL142106 | — | — | 1 | - |
| CHEMBL142153 | — | — | 1 | - |
| CHEMBL143853 | — | — | 1 | - |
| CHEMBL342994 | — | — | 1 | - |
| CHEMBL142224 | — | — | 1 | - |
| CHEMBL143824 | — | — | 1 | - |
| CHEMBL30054 | DPOC-4088 | 1.0 | 1 | - |
| CHEMBL145076 | — | — | 1 | - |
| CHEMBL347993 | — | — | 1 | - |
| CHEMBL342109 | — | — | 1 | - |
| CHEMBL143879 | — | — | 1 | - |
| CHEMBL143060 | — | — | 1 | - |
| CHEMBL143880 | — | — | 1 | - |
| CHEMBL143024 | — | — | 1 | - |
| CHEMBL142776 | — | — | 1 | - |
| CHEMBL142699 | — | — | 1 | - |
| CHEMBL141889 | — | — | 1 | - |
| CHEMBL142370 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL143418 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL143139 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL142546 | — | Ki | = | 855.0 | nM | 6.07 |
| CHEMBL142566 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL19080 | L-375378 | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL143138 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL143008 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL143421 | — | Ki | = | 4600.0 | nM | 5.34 |
| CHEMBL341909 | — | Ki | = | 40000.0 | nM | 4.40 |
| CHEMBL356296 | — | Ki | = | 47000.0 | nM | 4.33 |
| CHEMBL422299 | — | Ki | = | 61000.0 | nM | 4.21 |
| CHEMBL142240 | — | Ki | = | 80000.0 | nM | 4.10 |
| CHEMBL142106 | — | Ki | = | 136000.0 | nM | - |
| CHEMBL142153 | — | Ki | = | 270000.0 | nM | - |
| CHEMBL143853 | — | Ki | > | 1000000.0 | nM | - |
| CHEMBL342994 | — | Ki | = | 706000.0 | nM | - |
| CHEMBL142224 | — | Ki | = | 431000.0 | nM | - |
| CHEMBL143824 | — | Ki | = | 118000.0 | nM | - |
| CHEMBL30054 | DPOC-4088 | Ki | = | 202000.0 | nM | - |
| CHEMBL145076 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL347993 | — | Ki | = | 251000.0 | nM | - |
| CHEMBL342109 | — | Ki | = | 665000.0 | nM | - |
| CHEMBL143879 | — | Ki | = | 501000.0 | nM | - |
| CHEMBL143060 | — | Ki | > | 1000000.0 | nM | - |
| CHEMBL143880 | — | Ki | = | 898000.0 | nM | - |
| CHEMBL143024 | — | Ki | = | 213000.0 | nM | - |
| CHEMBL142776 | — | Ki | = | 567000.0 | nM | - |
| CHEMBL142699 | — | Ki | > | 1000000.0 | nM | - |
| CHEMBL141889 | — | Ki | = | 252000.0 | nM | - |
| CHEMBL142370 | — | Ki | = | 429000.0 | nM | - |