Assay Detail
Binding
CHEMBL5733207
Review assay metadata, readout intent, target linkage, and publication context from the same page.
FASN Inhibition: 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. The biochemical activities shown in TABLE 31 were determined using the fluorescence measurement of CoA release via a procedure described in Chung C. C. et al. (Assay and Drug Development Technologies, 2008, 6(3), 361-374).
1014
Total Activities
335
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Heterocyclic modulators of lipid synthesis and combinations thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 338 | 7.16 | 8.30 |
| kon | 338 | - | - |
| k_off | 338 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3962197 | — | — | 3 | 8.30 |
| CHEMBL3975955 | — | — | 3 | 8.22 |
| CHEMBL3915660 | — | — | 3 | 8.22 |
| CHEMBL3949918 | — | — | 3 | 8.15 |
| CHEMBL3968803 | — | — | 3 | 8.15 |
| CHEMBL3979428 | — | — | 3 | 8.10 |
| CHEMBL3927497 | — | — | 3 | 8.05 |
| CHEMBL3975941 | — | — | 3 | 8.05 |
| CHEMBL3940149 | — | — | 3 | 8.05 |
| CHEMBL3945625 | — | — | 3 | 8.05 |
| CHEMBL3960666 | — | — | 3 | 8.05 |
| CHEMBL3895704 | — | — | 3 | 8.05 |
| CHEMBL3922048 | — | — | 3 | 8.05 |
| CHEMBL3936614 | — | — | 3 | 8.05 |
| CHEMBL3906251 | — | — | 3 | 8.00 |
| CHEMBL3891794 | — | — | 3 | 8.00 |
| CHEMBL3935073 | — | — | 3 | 8.00 |
| CHEMBL3905299 | — | — | 3 | 8.00 |
| CHEMBL3902171 | — | — | 3 | 7.96 |
| CHEMBL3927676 | — | — | 3 | 7.96 |
| CHEMBL3936277 | — | — | 3 | 7.96 |
| CHEMBL3977044 | — | — | 3 | 7.96 |
| CHEMBL3908611 | — | — | 3 | 7.96 |
| CHEMBL3940947 | — | — | 3 | 7.96 |
| CHEMBL3894044 | — | — | 3 | 7.96 |
| CHEMBL3938270 | — | — | 3 | 7.96 |
| CHEMBL3973206 | — | — | 3 | 7.92 |
| CHEMBL3936004 | — | — | 3 | 7.92 |
| CHEMBL3986980 | — | — | 3 | 7.92 |
| CHEMBL3933162 | — | — | 3 | 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 |
| CHEMBL3960666 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3945625 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3936614 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3940149 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3895704 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3922048 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3975941 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3927497 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3906251 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3935073 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3905299 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3891794 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3908611 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3894044 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3977044 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3936277 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3940947 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3938270 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3902171 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3927676 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3933162 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3971866 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3973206 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3927639 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3916409 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3986980 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3936004 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3908686 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3960022 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3901281 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3893529 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3949269 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3899694 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3923215 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5839381 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3983146 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3978403 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3962560 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3971732 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3933878 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3965407 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3932624 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3919963 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3933609 | — | IC50 | = | 18.0 | nM | 7.75 |