Assay Detail
Binding
CHEMBL2162633
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal His8-tagged Bcl-XL expressed in Escherichia coli BL21(DE3) assessed as inhibition of Fluorescein-labeled BAK binding after 1 to 2 hrs by fluorescence polarization assay
30
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-based design of potent Bcl-2/Bcl-xL inhibitors with strong in vivo antitumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 6.15 | 8.92 |
| IC50 | 15 | 7.91 | 8.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2159738 | — | — | 2 | 8.92 |
| CHEMBL2159740 | — | — | 2 | 8.32 |
| CHEMBL2159743 | — | — | 2 | 8.30 |
| CHEMBL2159734 | — | — | 2 | 8.30 |
| CHEMBL2159737 | — | — | 2 | 8.22 |
| CHEMBL2159736 | — | — | 2 | 8.22 |
| CHEMBL376408 | ABT 737 | 1.0 | 2 | 8.22 |
| CHEMBL2159739 | — | — | 2 | 8.18 |
| CHEMBL2063897 | — | — | 2 | 8.12 |
| CHEMBL2159741 | — | — | 2 | 8.11 |
| CHEMBL2159735 | — | — | 2 | 8.05 |
| CHEMBL2159744 | — | — | 2 | 5.47 |
| CHEMBL2159733 | — | — | 2 | 4.06 |
| CHEMBL2159742 | — | — | 2 | - |
| CHEMBL2063880 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2159738 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL2159740 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL2159743 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2159734 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2159737 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL376408 | ABT 737 | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2159736 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2159739 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL2063897 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL2159741 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL2159735 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2159738 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2159744 | — | Ki | = | 3400.0 | nM | 5.47 |
| CHEMBL2159744 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL2159733 | — | Ki | = | 88000.0 | nM | 4.06 |
| CHEMBL2159742 | — | Ki | < | 1.0 | nM | - |
| CHEMBL2159741 | — | Ki | < | 1.0 | nM | - |
| CHEMBL2159740 | — | Ki | < | 1.0 | nM | - |
| CHEMBL2159739 | — | Ki | < | 1.0 | nM | - |
| CHEMBL2159737 | — | Ki | < | 1.0 | nM | - |
| CHEMBL2159736 | — | Ki | < | 1.0 | nM | - |
| CHEMBL376408 | ABT 737 | Ki | < | 1.0 | nM | - |
| CHEMBL2159735 | — | Ki | < | 1.0 | nM | - |
| CHEMBL2159734 | — | Ki | < | 1.0 | nM | - |
| CHEMBL2063897 | — | Ki | < | 1.0 | nM | - |
| CHEMBL2159742 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL2159733 | — | IC50 | = | 291000.0 | nM | - |
| CHEMBL2063880 | — | IC50 | = | 453000.0 | nM | - |
| CHEMBL2063880 | — | Ki | = | 138000.0 | nM | - |
| CHEMBL2159743 | — | Ki | < | 1.0 | nM | - |