Assay Detail
Binding
CHEMBL1961308
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Competitive inhibition of human aromatase using dibenzylfluorescein substrate after 10 mins preincubation measured every 10 sec for 5 mins by Michaelis-Menten and Dixon plot analysis
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimization of the aromatase inhibitory activities of pyridylthiazole analogues of resveratrol.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.20 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1444 | LETROZOLE | 4.0 | 1 | 10.70 |
| CHEMBL9298 | FADROZOLE | 2.0 | 1 | 10.30 |
| CHEMBL1957214 | — | — | 1 | 10.22 |
| CHEMBL1399 | ANASTROZOLE | 4.0 | 1 | 9.89 |
| CHEMBL1957217 | — | — | 1 | 9.19 |
| CHEMBL1957218 | — | — | 1 | 8.50 |
| CHEMBL1957216 | — | — | 1 | 8.09 |
| CHEMBL1957223 | — | — | 1 | 7.45 |
| CHEMBL1601919 | — | — | 1 | 7.20 |
| CHEMBL1957221 | — | — | 1 | 7.08 |
| CHEMBL1957222 | — | — | 1 | 7.00 |
| CHEMBL1957211 | — | — | 1 | 6.63 |
| CHEMBL1957219 | — | — | 1 | 6.54 |
| CHEMBL1957208 | — | — | 1 | 5.94 |
| CHEMBL1957220 | — | — | 1 | 5.83 |
| CHEMBL1957212 | — | — | 1 | 5.76 |
| CHEMBL1957215 | — | — | 1 | 5.59 |
| CHEMBL1957209 | — | — | 1 | 5.27 |
| CHEMBL1957210 | — | — | 1 | 4.90 |
| CHEMBL1957213 | — | — | 1 | 4.82 |
| CHEMBL165 | RESVERATROL | 3.0 | 1 | 4.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1444 | LETROZOLE | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL9298 | FADROZOLE | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL1957214 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL1399 | ANASTROZOLE | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL1957217 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL1957218 | — | Ki | = | 3.17 | nM | 8.50 |
| CHEMBL1957216 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL1957223 | — | Ki | = | 35.12 | nM | 7.45 |
| CHEMBL1601919 | — | Ki | = | 63.38 | nM | 7.20 |
| CHEMBL1957221 | — | Ki | = | 82.54 | nM | 7.08 |
| CHEMBL1957222 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL1957211 | — | Ki | = | 234.3 | nM | 6.63 |
| CHEMBL1957219 | — | Ki | = | 285.1 | nM | 6.54 |
| CHEMBL1957208 | — | Ki | = | 1160.0 | nM | 5.94 |
| CHEMBL1957220 | — | Ki | = | 1482.0 | nM | 5.83 |
| CHEMBL1957212 | — | Ki | = | 1722.0 | nM | 5.76 |
| CHEMBL1957215 | — | Ki | = | 2548.0 | nM | 5.59 |
| CHEMBL1957209 | — | Ki | = | 5321.0 | nM | 5.27 |
| CHEMBL1957210 | — | Ki | = | 12560.0 | nM | 4.90 |
| CHEMBL1957213 | — | Ki | = | 15000.0 | nM | 4.82 |
| CHEMBL165 | RESVERATROL | Ki | = | 41670.0 | nM | 4.38 |