Assay Detail
Binding
CHEMBL3789523
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Inhibition of Hh signaling pathway in mouse TM3 cells assessed as downregulation of Gli1 gene expression after 48 hrs by luciferase reporter gene assay
33
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | TM3 |
| Confidence | 3 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Development of thieno- and benzopyrimidinone inhibitors of the Hedgehog signaling pathway reveals PDE4-dependent and PDE4-independent mechanisms of action.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 33 | 5.88 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2105737 | SONIDEGIB | 4.0 | 1 | 8.92 |
| CHEMBL473417 | VISMODEGIB | 4.0 | 1 | 7.89 |
| CHEMBL3785925 | — | — | 1 | 7.09 |
| CHEMBL3785859 | — | — | 1 | 6.32 |
| CHEMBL3787601 | — | — | 1 | 6.16 |
| CHEMBL3787120 | — | — | 1 | 6.03 |
| CHEMBL3787562 | — | — | 1 | 6.03 |
| CHEMBL3785184 | — | — | 1 | 6.02 |
| CHEMBL3786351 | — | — | 1 | 5.94 |
| CHEMBL3785585 | — | — | 1 | 5.89 |
| CHEMBL3785098 | — | — | 2 | 5.87 |
| CHEMBL3786800 | — | — | 1 | 5.72 |
| CHEMBL3786264 | — | — | 1 | 5.70 |
| CHEMBL3787593 | — | — | 1 | 5.68 |
| CHEMBL3786592 | — | — | 1 | 5.63 |
| CHEMBL3785931 | — | — | 1 | 5.63 |
| CHEMBL3787553 | — | — | 1 | 5.34 |
| CHEMBL1334234 | — | — | 1 | 5.24 |
| CHEMBL3787667 | — | — | 1 | 5.19 |
| CHEMBL3787302 | — | — | 1 | 5.08 |
| CHEMBL471728 | — | — | 1 | 5.03 |
| CHEMBL3785488 | — | — | 1 | 4.97 |
| CHEMBL3786377 | — | — | 1 | 4.96 |
| CHEMBL3786034 | — | — | 1 | 4.70 |
| CHEMBL3785965 | — | — | 1 | - |
| CHEMBL3785441 | — | — | 1 | - |
| CHEMBL3787149 | — | — | 1 | - |
| CHEMBL3787551 | — | — | 1 | - |
| CHEMBL3785218 | — | — | 1 | - |
| CHEMBL3787130 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2105737 | SONIDEGIB | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL473417 | VISMODEGIB | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3785925 | — | EC50 | = | 82.0 | nM | 7.09 |
| CHEMBL3785859 | — | EC50 | = | 481.0 | nM | 6.32 |
| CHEMBL3787601 | — | EC50 | = | 685.0 | nM | 6.16 |
| CHEMBL3787120 | — | EC50 | = | 933.0 | nM | 6.03 |
| CHEMBL3787562 | — | EC50 | = | 931.0 | nM | 6.03 |
| CHEMBL3785184 | — | EC50 | = | 948.0 | nM | 6.02 |
| CHEMBL3786351 | — | EC50 | = | 1160.0 | nM | 5.94 |
| CHEMBL3785585 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3785098 | — | EC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL3786800 | — | EC50 | = | 1890.0 | nM | 5.72 |
| CHEMBL3786264 | — | EC50 | = | 1990.0 | nM | 5.70 |
| CHEMBL3787593 | — | EC50 | = | 2070.0 | nM | 5.68 |
| CHEMBL3785931 | — | EC50 | = | 2360.0 | nM | 5.63 |
| CHEMBL3786592 | — | EC50 | = | 2320.0 | nM | 5.63 |
| CHEMBL3787553 | — | EC50 | = | 4570.0 | nM | 5.34 |
| CHEMBL1334234 | — | EC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL3787667 | — | EC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL3787302 | — | EC50 | = | 8250.0 | nM | 5.08 |
| CHEMBL471728 | — | EC50 | = | 9270.0 | nM | 5.03 |
| CHEMBL3785488 | — | EC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL3786377 | — | EC50 | = | 11100.0 | nM | 4.96 |
| CHEMBL3786034 | — | EC50 | = | 19800.0 | nM | 4.70 |
| CHEMBL3785965 | — | EC50 | > | 20000.0 | nM | - |
| CHEMBL3785441 | — | EC50 | > | 20000.0 | nM | - |
| CHEMBL3787149 | — | EC50 | > | 20000.0 | nM | - |
| CHEMBL3787551 | — | EC50 | > | 20000.0 | nM | - |
| CHEMBL3785218 | — | EC50 | > | 20000.0 | nM | - |
| CHEMBL3785098 | — | EC50 | < | 1000.0 | nM | - |
| CHEMBL3787130 | — | EC50 | > | 20000.0 | nM | - |
| CHEMBL3785251 | — | EC50 | > | 20000.0 | nM | - |
| CHEMBL3785982 | — | EC50 | > | 20000.0 | nM | - |