Assay Detail
Binding
CHEMBL3406793
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Inhibition of GST-tagged Bcl-xL (unknown origin) measured after 1 hr incubation by fluorescence polarization assay
26
Total Activities
26
Compounds Tested
4
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
A combination of in silico and SAR studies to identify binding hot spots of Bcl-xL inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.50 | 8.82 |
| Ki | 9 | 6.31 | 7.77 |
| Activity | 3 | - | - |
| Kd | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3400497 | — | — | 1 | 8.82 |
| CHEMBL3342187 | — | — | 1 | 8.52 |
| CHEMBL1689139 | — | — | 1 | 8.52 |
| CHEMBL3126119 | — | — | 1 | 8.36 |
| CHEMBL376408 | ABT 737 | 1.0 | 1 | 8.22 |
| CHEMBL3400495 | — | — | 1 | 8.22 |
| CHEMBL1236741 | — | — | 1 | 7.96 |
| CHEMBL2030861 | — | — | 1 | 7.89 |
| CHEMBL3400492 | — | — | 1 | 7.77 |
| CHEMBL3287282 | — | — | 1 | 7.68 |
| CHEMBL371861 | — | — | 1 | 7.44 |
| CHEMBL1374578 | — | — | 1 | 6.30 |
| CHEMBL3400496 | — | — | 1 | 6.30 |
| CHEMBL3400491 | — | — | 1 | 6.03 |
| CHEMBL51483 | GOSSYPOL | 3.0 | 1 | 6.00 |
| CHEMBL3400494 | — | — | 1 | 5.96 |
| CHEMBL335265 | — | — | 1 | 5.62 |
| CHEMBL3400493 | — | — | 1 | 5.39 |
| CHEMBL3125476 | — | — | 1 | 4.89 |
| CHEMBL3125475 | — | — | 1 | 4.66 |
| CHEMBL2063880 | — | — | 1 | - |
| CHEMBL106708 | — | — | 1 | - |
| CHEMBL1230221 | — | — | 1 | - |
| CHEMBL218222 | — | — | 1 | - |
| CHEMBL218223 | — | — | 1 | - |
| CHEMBL449132 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3400497 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3342187 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1689139 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3126119 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL376408 | ABT 737 | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3400495 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1236741 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2030861 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3400492 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL3287282 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL371861 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL1374578 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL3400496 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3400491 | — | Ki | = | 930.0 | nM | 6.03 |
| CHEMBL51483 | GOSSYPOL | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL3400494 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL335265 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL3400493 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL3125476 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL3125475 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL2063880 | — | Ki | = | 138000.0 | nM | - |
| CHEMBL106708 | — | Kd | = | 300000.0 | nM | - |
| CHEMBL1230221 | — | Activity | - | — | - | |
| CHEMBL218222 | — | Activity | - | — | - | |
| CHEMBL218223 | — | Activity | - | — | - | |
| CHEMBL449132 | — | Kd | = | 4300000.0 | nM | - |