Assay Detail
Binding
CHEMBL3888977
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Biochemical Assay: The FASN enzyme was isolated from SKBr3 cells. SKBr3 is a human breast cancer cell-line with high levels of FASN expression. It is estimated that FASN comprises about 25% of the cytosolic proteins in this cell line. SKBr3 cells were homogenized in a dounce homogenizer then centrifuged for 15 minutes at 4° C. to remove particulate matter. The supernatant was then analyzed for protein content, diluted to the appropriate concentration, and used to measure FASN activity. The presence of FASN was confirmed by western blot analysis. A similar method for isolation of FASN from SKBr3 cells is described in Teresa, P. et al. (Clin. Cancer Res. 2009; 15(24), 7608-7615). FASN activity of the SKBr3 cell extract was determined by measuring either NADPH oxidation or the amount of thiol-containing coenzyme A (CoA) released during the fatty acid synthase reaction. The dye CPM (7-diethylamino-3-(4'-maleimidyl-phenyl)-4-methylcoumarin) contains a thiol reactive group that increases its fluorescence emission on reaction with the sulfhydryl group of CoA.
338
Total Activities
334
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Cancer cell lines |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Heterocyclic modulators of lipid synthesis
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 338 | 7.16 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3962197 | — | — | 1 | 8.30 |
| CHEMBL3975955 | — | — | 1 | 8.22 |
| CHEMBL3915660 | — | — | 1 | 8.22 |
| CHEMBL3949918 | — | — | 1 | 8.15 |
| CHEMBL3968803 | — | — | 1 | 8.15 |
| CHEMBL3979428 | — | — | 1 | 8.10 |
| CHEMBL3927497 | — | — | 1 | 8.05 |
| CHEMBL3975941 | — | — | 1 | 8.05 |
| CHEMBL3940149 | — | — | 1 | 8.05 |
| CHEMBL3945625 | — | — | 1 | 8.05 |
| CHEMBL3960666 | — | — | 1 | 8.05 |
| CHEMBL3895704 | — | — | 1 | 8.05 |
| CHEMBL3922048 | — | — | 1 | 8.05 |
| CHEMBL3936614 | — | — | 1 | 8.05 |
| CHEMBL3906251 | — | — | 1 | 8.00 |
| CHEMBL3891794 | — | — | 1 | 8.00 |
| CHEMBL3935073 | — | — | 1 | 8.00 |
| CHEMBL3905299 | — | — | 1 | 8.00 |
| CHEMBL3902171 | — | — | 1 | 7.96 |
| CHEMBL3927676 | — | — | 1 | 7.96 |
| CHEMBL3936277 | — | — | 1 | 7.96 |
| CHEMBL3977044 | — | — | 1 | 7.96 |
| CHEMBL3908611 | — | — | 1 | 7.96 |
| CHEMBL3940947 | — | — | 1 | 7.96 |
| CHEMBL3894044 | — | — | 1 | 7.96 |
| CHEMBL3938270 | — | — | 1 | 7.96 |
| CHEMBL3973206 | — | — | 1 | 7.92 |
| CHEMBL3936004 | — | — | 1 | 7.92 |
| CHEMBL3986980 | — | — | 1 | 7.92 |
| CHEMBL3933162 | — | — | 1 | 7.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3962197 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3975955 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3915660 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3968803 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3949918 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3979428 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3975941 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3960666 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3927497 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3936614 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3940149 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3945625 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3922048 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3895704 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3935073 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3905299 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3891794 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3906251 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3902171 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3977044 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3938270 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3936277 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3894044 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3908611 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3940947 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3927676 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3986980 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3936004 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3933162 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3973206 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3971866 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3927639 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3916409 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3901281 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3908686 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3960022 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3893529 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3923215 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3949269 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3899694 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3983146 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3965791 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3933878 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3962560 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3978403 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3971732 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3932624 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3919963 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3917458 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3985588 | — | IC50 | = | 18.0 | nM | 7.75 |