Assay Detail
ADMET
CHEMBL1038133
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Inhibition of human CYP3A4 in human liver microsomes preincubated with NADPH
14
Total Activities
14
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 | Intermediate |
Publication
Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.00 | 5.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL494979 | — | — | 1 | 5.70 |
| CHEMBL585293 | — | — | 1 | 5.41 |
| CHEMBL496102 | AMG-208 | 2.0 | 1 | 5.39 |
| CHEMBL567908 | — | — | 1 | 5.32 |
| CHEMBL522196 | — | — | 1 | 5.19 |
| CHEMBL567089 | — | — | 1 | 5.16 |
| CHEMBL494630 | — | — | 1 | 5.08 |
| CHEMBL566253 | — | — | 1 | 5.05 |
| CHEMBL566242 | — | — | 1 | 5.04 |
| CHEMBL565843 | — | — | 1 | 4.80 |
| CHEMBL566685 | — | — | 1 | 4.58 |
| CHEMBL568138 | — | — | 1 | 4.54 |
| CHEMBL566875 | — | — | 1 | 4.39 |
| CHEMBL566683 | — | — | 1 | 4.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL494979 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL585293 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL496102 | AMG-208 | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL567908 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL522196 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL567089 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL494630 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL566253 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL566242 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL565843 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL566685 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL568138 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL566875 | — | IC50 | = | 41000.0 | nM | 4.39 |
| CHEMBL566683 | — | IC50 | = | 50000.0 | nM | 4.30 |