Assay Detail
Binding
CHEMBL2162634
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal His8-tagged Mcl1 expressed in Escherichia coli BL21(DE3) assessed as inhibition of Fluorescein-labeled BID binding after 1 to 2 hrs by fluorescence polarization assay
15
Total Activities
15
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 |
Target
Induced myeloid leukemia cell differentiation protein Mcl-1 (CHEMBL4361) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 |
|---|---|---|---|
| IC50 | 15 | 6.74 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2159742 | — | — | 1 | 8.30 |
| CHEMBL2159744 | — | — | 1 | 7.43 |
| CHEMBL2159743 | — | — | 1 | 4.50 |
| CHEMBL2159736 | — | — | 1 | - |
| CHEMBL2159735 | — | — | 1 | - |
| CHEMBL376408 | ABT 737 | 1.0 | 1 | - |
| CHEMBL2159741 | — | — | 1 | - |
| CHEMBL2159740 | — | — | 1 | - |
| CHEMBL2159739 | — | — | 1 | - |
| CHEMBL2159737 | — | — | 1 | - |
| CHEMBL2063897 | — | — | 1 | - |
| CHEMBL2159734 | — | — | 1 | - |
| CHEMBL2159733 | — | — | 1 | - |
| CHEMBL2063880 | — | — | 1 | - |
| CHEMBL2159738 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2159742 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2159744 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL2159743 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL2159736 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2159735 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL376408 | ABT 737 | IC50 | > | 1000.0 | nM | - |
| CHEMBL2159741 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL2159740 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL2159739 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL2159737 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL2063897 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL2159734 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2159733 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2063880 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2159738 | — | IC50 | > | 10000.0 | nM | - |