Assay Detail
Binding
CHEMBL4276234
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Inhibition of recombinant His6-tagged BRG1 ATPase-SnAC (658 to 1361 residues) (unknown origin) expressed in insect sf9 cells preincubated for 5 mins followed by pCMV-dR8.91 plasmid and ATP addition measured after 60 mins by ADP-Glo assay
14
Total Activities
14
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
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 |
|---|---|---|---|
| IC50 | 14 | 7.03 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4278436 | — | — | 1 | 8.22 |
| CHEMBL4294655 | — | — | 1 | 8.00 |
| CHEMBL4286757 | — | — | 1 | 7.52 |
| CHEMBL4290175 | — | — | 1 | 7.52 |
| CHEMBL4281368 | — | — | 1 | 6.82 |
| CHEMBL4282784 | — | — | 1 | 6.24 |
| CHEMBL4290675 | — | — | 1 | 6.11 |
| CHEMBL4292870 | — | — | 1 | 5.77 |
| CHEMBL4295096 | — | — | 1 | - |
| CHEMBL4282980 | — | — | 1 | - |
| CHEMBL4293567 | — | — | 1 | - |
| CHEMBL4286345 | — | — | 1 | - |
| CHEMBL4279505 | — | — | 1 | - |
| CHEMBL4291666 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4278436 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4294655 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4286757 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4290175 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4281368 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4282784 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4290675 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL4292870 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4295096 | — | IC50 | < | 5.0 | nM | - |
| CHEMBL4282980 | — | IC50 | < | 5.0 | nM | - |
| CHEMBL4293567 | — | IC50 | < | 5.0 | nM | - |
| CHEMBL4286345 | — | IC50 | < | 5.0 | nM | - |
| CHEMBL4279505 | — | IC50 | - | — | - | |
| CHEMBL4291666 | — | IC50 | - | — | - |