Assay Detail
Binding
CHEMBL3411198
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of purified recombinant FASN TE activity (unknown origin) using 4-MUH as substrate preincubated for 30 mins before substrate addition measured after 1 hr by fluorescence assay
11
Total Activities
6
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Repositioning proton pump inhibitors as anticancer drugs by targeting the thioesterase domain of human fatty acid synthase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 4.40 | 4.53 |
| Ki | 4 | 5.34 | 5.47 |
| Inhibition | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1503 | OMEPRAZOLE | 4.0 | 2 | 5.47 |
| CHEMBL1502 | PANTOPRAZOLE | 4.0 | 3 | 5.39 |
| CHEMBL480 | LANSOPRAZOLE | 4.0 | 2 | 5.28 |
| CHEMBL1219 | RABEPRAZOLE | 4.0 | 2 | 5.23 |
| CHEMBL547 | ISOTRETINOIN | 4.0 | 1 | - |
| CHEMBL404849 | SULOCTIDIL | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1503 | OMEPRAZOLE | Ki | = | 3400.0 | nM | 5.47 |
| CHEMBL1502 | PANTOPRAZOLE | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL480 | LANSOPRAZOLE | Ki | = | 5300.0 | nM | 5.28 |
| CHEMBL1219 | RABEPRAZOLE | Ki | = | 5900.0 | nM | 5.23 |
| CHEMBL1503 | OMEPRAZOLE | IC50 | = | 29600.0 | nM | 4.53 |
| CHEMBL1502 | PANTOPRAZOLE | IC50 | = | 36200.0 | nM | 4.44 |
| CHEMBL480 | LANSOPRAZOLE | IC50 | = | 46700.0 | nM | 4.33 |
| CHEMBL1219 | RABEPRAZOLE | IC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL1502 | PANTOPRAZOLE | Inhibition | >= | 40.0 | % | - |
| CHEMBL547 | ISOTRETINOIN | Inhibition | >= | 40.0 | % | - |
| CHEMBL404849 | SULOCTIDIL | Inhibition | >= | 40.0 | % | - |