Assay Detail
Binding
CHEMBL4041201
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-cyclopamine from SMO V404M mutant in gefitinib resistant human HCC827 cells by scintillation counting
10
Total Activities
10
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
Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.22 | 7.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL473417 | VISMODEGIB | 4.0 | 1 | 7.91 |
| CHEMBL1852688 | INFIGRATINIB | 4.0 | 1 | 7.33 |
| CHEMBL386051 | — | — | 1 | 7.33 |
| CHEMBL4105444 | — | — | 1 | 7.30 |
| CHEMBL254129 | CYCLOPAMINE | — | 1 | 7.29 |
| CHEMBL254760 | — | — | 1 | 7.28 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 7.17 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 7.06 |
| CHEMBL1796172 | — | — | 1 | 6.77 |
| CHEMBL2029988 | CEP-32496 | 2.0 | 1 | 6.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL473417 | VISMODEGIB | Ki | = | 12.2 | nM | 7.91 |
| CHEMBL1852688 | INFIGRATINIB | Ki | = | 46.5 | nM | 7.33 |
| CHEMBL386051 | — | Ki | = | 46.2 | nM | 7.33 |
| CHEMBL4105444 | — | Ki | = | 50.4 | nM | 7.30 |
| CHEMBL254129 | CYCLOPAMINE | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL254760 | — | Ki | = | 53.1 | nM | 7.28 |
| CHEMBL1230609 | FORETINIB | Ki | = | 66.8 | nM | 7.17 |
| CHEMBL223360 | LINIFANIB | Ki | = | 87.6 | nM | 7.06 |
| CHEMBL1796172 | — | Ki | = | 168.1 | nM | 6.77 |
| CHEMBL2029988 | CEP-32496 | Ki | = | 187.8 | nM | 6.73 |