Assay Detail
ADMET
CHEMBL666015
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Inhibition of human Cytochrome P450 3A4 by macrocycles
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.33 | 6.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL312137 | — | — | 1 | 6.00 |
| CHEMBL526656 | — | — | 1 | 5.55 |
| CHEMBL312121 | — | — | 1 | 5.30 |
| CHEMBL80702 | — | — | 1 | 5.22 |
| CHEMBL311561 | — | — | 1 | 5.21 |
| CHEMBL526466 | — | — | 1 | 5.18 |
| CHEMBL53821 | — | — | 1 | 5.10 |
| CHEMBL502560 | — | — | 1 | 5.05 |
| CHEMBL310586 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL312137 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL526656 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL312121 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL80702 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL311561 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL526466 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL53821 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL502560 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL310586 | — | IC50 | < | 50.0 | nM | - |