Assay Detail
Binding
CHEMBL4041200
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Displacement of [3H]-cyclopamine from human wild-type SMO receptor expressed in HEK293T cell membranes by liquid scintillation spectrometry
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| 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 | 14 | 7.30 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL254760 | — | — | 1 | 7.38 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 7.22 |
| CHEMBL1614725 | TAK-285 | 1.0 | 1 | - |
| CHEMBL1779065 | — | — | 1 | - |
| CHEMBL1796172 | — | — | 1 | - |
| CHEMBL4101154 | — | — | 1 | - |
| CHEMBL460702 | BMS-777607 | 2.0 | 1 | - |
| CHEMBL1852688 | INFIGRATINIB | 4.0 | 1 | - |
| CHEMBL2029988 | CEP-32496 | 2.0 | 1 | - |
| CHEMBL4105444 | — | — | 1 | - |
| CHEMBL386051 | — | — | 1 | - |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | - |
| CHEMBL254129 | CYCLOPAMINE | — | 1 | - |
| CHEMBL473417 | VISMODEGIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL254760 | — | Ki | = | 41.7 | nM | 7.38 |
| CHEMBL1230609 | FORETINIB | Ki | = | 59.7 | nM | 7.22 |
| CHEMBL1614725 | TAK-285 | Ki | - | — | - | |
| CHEMBL1779065 | — | Ki | - | — | - | |
| CHEMBL1796172 | — | Ki | - | — | - | |
| CHEMBL4101154 | — | Ki | - | — | - | |
| CHEMBL460702 | BMS-777607 | Ki | - | — | - | |
| CHEMBL1852688 | INFIGRATINIB | Ki | - | — | - | |
| CHEMBL2029988 | CEP-32496 | Ki | - | — | - | |
| CHEMBL4105444 | — | Ki | - | — | - | |
| CHEMBL386051 | — | Ki | - | — | - | |
| CHEMBL223360 | LINIFANIB | Ki | - | — | - | |
| CHEMBL254129 | CYCLOPAMINE | Ki | - | — | - | |
| CHEMBL473417 | VISMODEGIB | Ki | - | — | - |