Assay Detail
Binding
CHEMBL4276242
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Inhibition of BRM/BRG1 mutant in human NCI-H1299 cells assessed as reduction in KRT80 gene expression after 24 hrs by luciferase reporter gene assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | NCI-H1299 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 7 | 7.24 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4295096 | — | — | 1 | 8.00 |
| CHEMBL4282980 | — | — | 1 | 8.00 |
| CHEMBL4286345 | — | — | 1 | 7.58 |
| CHEMBL4293567 | — | — | 1 | 7.38 |
| CHEMBL4278436 | — | — | 1 | 6.44 |
| CHEMBL4294655 | — | — | 1 | 6.03 |
| CHEMBL4286757 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4295096 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4282980 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4286345 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4293567 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4278436 | — | EC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4294655 | — | EC50 | = | 930.0 | nM | 6.03 |
| CHEMBL4286757 | — | EC50 | > | 10000.0 | nM | - |