Assay Detail
ADMET
CHEMBL4002822
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Inhibition of platelet NHE1 in human platelet rich plasma assessed as decrease in platelet swelling preincubated for 3 mins followed by sodium propionate addition measured after 4 mins by spectrophotometric method
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Sodium hydrogen exchanger inhibitory activity of benzotriazole derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 4.36 | 6.76 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL436559 | CARIPORIDE | 2.0 | 1 | 6.76 |
| CHEMBL4071353 | — | — | 1 | 4.30 |
| CHEMBL4095965 | — | — | 1 | 4.29 |
| CHEMBL1288725 | — | — | 1 | 4.29 |
| CHEMBL4082866 | — | — | 1 | 4.23 |
| CHEMBL4072374 | — | — | 1 | 4.22 |
| CHEMBL557236 | — | — | 1 | 4.20 |
| CHEMBL4074684 | — | — | 1 | 4.19 |
| CHEMBL945 | AMILORIDE | 4.0 | 1 | 4.18 |
| CHEMBL425230 | — | — | 1 | 4.17 |
| CHEMBL4084954 | — | — | 1 | 4.16 |
| CHEMBL1884989 | — | — | 1 | 4.14 |
| CHEMBL204234 | — | — | 1 | 4.14 |
| CHEMBL4097403 | — | — | 1 | 4.06 |
| CHEMBL3086212 | — | — | 1 | 4.01 |
| CHEMBL4085368 | — | — | 1 | - |
| CHEMBL4093129 | — | — | 1 | - |
| CHEMBL4072288 | — | — | 1 | - |
| CHEMBL4087253 | — | — | 1 | - |
| CHEMBL4079373 | — | — | 1 | - |
| CHEMBL4068558 | — | — | 1 | - |
| CHEMBL84963 | BENZOTRIAZOLE | — | 1 | - |
| CHEMBL4100842 | — | — | 1 | - |
| CHEMBL4063302 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL436559 | CARIPORIDE | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL4071353 | — | IC50 | = | 49950.0 | nM | 4.30 |
| CHEMBL4095965 | — | IC50 | = | 50890.0 | nM | 4.29 |
| CHEMBL1288725 | — | IC50 | = | 51570.0 | nM | 4.29 |
| CHEMBL4082866 | — | IC50 | = | 59230.0 | nM | 4.23 |
| CHEMBL4072374 | — | IC50 | = | 60590.0 | nM | 4.22 |
| CHEMBL557236 | — | IC50 | = | 63470.0 | nM | 4.20 |
| CHEMBL4074684 | — | IC50 | = | 65140.0 | nM | 4.19 |
| CHEMBL945 | AMILORIDE | IC50 | = | 66730.0 | nM | 4.18 |
| CHEMBL425230 | — | IC50 | = | 68110.0 | nM | 4.17 |
| CHEMBL4084954 | — | IC50 | = | 69750.0 | nM | 4.16 |
| CHEMBL1884989 | — | IC50 | = | 72510.0 | nM | 4.14 |
| CHEMBL204234 | — | IC50 | = | 72380.0 | nM | 4.14 |
| CHEMBL4097403 | — | IC50 | = | 86480.0 | nM | 4.06 |
| CHEMBL3086212 | — | IC50 | = | 97100.0 | nM | 4.01 |
| CHEMBL4085368 | — | IC50 | = | 191230.0 | nM | - |
| CHEMBL4093129 | — | IC50 | = | 154670.0 | nM | - |
| CHEMBL4072288 | — | IC50 | = | 101120.0 | nM | - |
| CHEMBL4087253 | — | IC50 | = | 135000.0 | nM | - |
| CHEMBL4079373 | — | IC50 | = | 355000.0 | nM | - |
| CHEMBL4068558 | — | IC50 | = | 177000.0 | nM | - |
| CHEMBL84963 | BENZOTRIAZOLE | IC50 | = | 192680.0 | nM | - |
| CHEMBL4100842 | — | IC50 | = | 156540.0 | nM | - |
| CHEMBL4063302 | — | IC50 | = | 115250.0 | nM | - |