Assay Detail
Binding
CHEMBL2015040
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Inhibition of CYP1A1 activity in rat liver microsomes using benzo[alpha]pyrene as substrate after 10 mins by fluorescence analysis
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and structure elucidation of novel fused 1,2,4-triazine derivatives as potent inhibitors targeting CYP1A1 activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.91 | 8.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2013099 | — | — | 1 | 8.27 |
| CHEMBL2013100 | — | — | 1 | 8.26 |
| CHEMBL2013097 | — | — | 1 | 8.24 |
| CHEMBL2013098 | — | — | 1 | 8.18 |
| CHEMBL2013101 | — | — | 1 | 8.11 |
| CHEMBL2013096 | — | — | 1 | 8.08 |
| CHEMBL2013093 | — | — | 1 | 8.01 |
| CHEMBL2013094 | — | — | 1 | 7.98 |
| CHEMBL2013095 | — | — | 1 | 7.88 |
| CHEMBL2013091 | — | — | 1 | 7.62 |
| CHEMBL2013102 | — | — | 1 | 7.21 |
| CHEMBL2013092 | — | — | 1 | 7.06 |
| CHEMBL2013090 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2013099 | — | IC50 | = | 5.42 | nM | 8.27 |
| CHEMBL2013100 | — | IC50 | = | 5.53 | nM | 8.26 |
| CHEMBL2013097 | — | IC50 | = | 5.69 | nM | 8.24 |
| CHEMBL2013098 | — | IC50 | = | 6.62 | nM | 8.18 |
| CHEMBL2013101 | — | IC50 | = | 7.74 | nM | 8.11 |
| CHEMBL2013096 | — | IC50 | = | 8.36 | nM | 8.08 |
| CHEMBL2013093 | — | IC50 | = | 9.71 | nM | 8.01 |
| CHEMBL2013094 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL2013095 | — | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL2013091 | — | IC50 | = | 24.2 | nM | 7.62 |
| CHEMBL2013102 | — | IC50 | = | 61.4 | nM | 7.21 |
| CHEMBL2013092 | — | IC50 | = | 86.7 | nM | 7.06 |
| CHEMBL2013090 | — | IC50 | - | — | - |