Assay Detail
Binding
CHEMBL4817528
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ASM in dog MDCK cells co-expressing recombinant full length mGFP-tagged KRAS G12V mutant and mCherry-CAAX assessed as reduction in plasma membrane localization of KRAS mutant incubated for 48 hrs by confocal microscopic analysis
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Canis lupus familiaris |
| Cell Type | MDCK |
| Subcellular | Plasma Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Scaffold repurposing of fendiline: Identification of potent KRAS plasma membrane localization inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 5.68 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4854753 | — | — | 1 | 7.70 |
| CHEMBL4858481 | — | — | 1 | 7.00 |
| CHEMBL4878364 | — | — | 1 | 6.70 |
| CHEMBL4859726 | — | — | 1 | 6.52 |
| CHEMBL4849536 | — | — | 1 | 6.30 |
| CHEMBL4868505 | — | — | 1 | 6.30 |
| CHEMBL4871394 | — | — | 1 | 6.22 |
| CHEMBL4859822 | — | — | 1 | 6.22 |
| CHEMBL4876631 | — | — | 1 | 5.96 |
| CHEMBL4878842 | — | — | 1 | 5.92 |
| CHEMBL4851942 | — | — | 1 | 5.92 |
| CHEMBL4847178 | — | — | 1 | 5.89 |
| CHEMBL4862403 | — | — | 1 | 5.82 |
| CHEMBL4864189 | — | — | 1 | 5.55 |
| CHEMBL4871910 | — | — | 1 | 5.48 |
| CHEMBL4870504 | — | — | 1 | 5.42 |
| CHEMBL4858212 | — | — | 1 | 5.42 |
| CHEMBL4862663 | — | — | 1 | 5.36 |
| CHEMBL4851435 | — | — | 1 | 5.28 |
| CHEMBL4871115 | — | — | 1 | 5.15 |
| CHEMBL4861239 | — | — | 1 | 5.11 |
| CHEMBL4850799 | — | — | 1 | 5.00 |
| CHEMBL4846949 | — | — | 1 | 4.97 |
| CHEMBL4867468 | — | — | 1 | 4.95 |
| CHEMBL4875085 | — | — | 1 | 4.95 |
| CHEMBL4854899 | — | — | 1 | 4.89 |
| CHEMBL4845855 | — | — | 1 | 4.83 |
| CHEMBL4867441 | — | — | 1 | 4.23 |
| CHEMBL4860440 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4854753 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4858481 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4878364 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4859726 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4849536 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4868505 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4871394 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4859822 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4876631 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4878842 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4851942 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4847178 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4862403 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4864189 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4871910 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4870504 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4858212 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4862663 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL4851435 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL4871115 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL4861239 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL4850799 | — | IC50 | = | 10100.0 | nM | 5.00 |
| CHEMBL4846949 | — | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL4867468 | — | IC50 | = | 11200.0 | nM | 4.95 |
| CHEMBL4875085 | — | IC50 | = | 11200.0 | nM | 4.95 |
| CHEMBL4854899 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4845855 | — | IC50 | = | 14800.0 | nM | 4.83 |
| CHEMBL4867441 | — | IC50 | = | 59300.0 | nM | 4.23 |
| CHEMBL4860440 | — | IC50 | - | — | - |