Assay Detail
ADMET
CHEMBL1228481
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Inhibition of CYP3A4 in human liver microsomes
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Tissue | Liver |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
The synthesis and structure-activity relationship of 4-benzimidazolyl-piperidinylcarbonyl-piperidine analogs as histamine H3 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 5.55 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1223002 | — | — | 1 | 6.70 |
| CHEMBL1222940 | — | — | 1 | 6.52 |
| CHEMBL1223001 | — | — | 1 | 6.40 |
| CHEMBL1222938 | — | — | 1 | 6.40 |
| CHEMBL1223003 | — | — | 1 | 6.40 |
| CHEMBL1222939 | — | — | 1 | 6.30 |
| CHEMBL1222650 | — | — | 1 | 5.82 |
| CHEMBL1222719 | — | — | 1 | 5.22 |
| CHEMBL1222649 | — | — | 1 | 5.12 |
| CHEMBL1222798 | — | — | 1 | 5.05 |
| CHEMBL1222485 | — | — | 1 | 5.02 |
| CHEMBL1222799 | — | — | 1 | 4.97 |
| CHEMBL1222717 | — | — | 1 | 4.96 |
| CHEMBL1222718 | — | — | 1 | 4.87 |
| CHEMBL1222863 | — | — | 1 | 4.52 |
| CHEMBL1222864 | — | — | 1 | 4.52 |
| CHEMBL1222800 | — | — | 1 | - |
| CHEMBL1222651 | — | — | 1 | - |
| CHEMBL1222865 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1223002 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1222940 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1223001 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL1222938 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL1223003 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL1222939 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1222650 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1222719 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL1222649 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL1222798 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL1222485 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL1222799 | — | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL1222717 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL1222718 | — | IC50 | = | 13500.0 | nM | 4.87 |
| CHEMBL1222863 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL1222864 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL1222800 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1222651 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1222865 | — | IC50 | > | 30000.0 | nM | - |