Assay Detail
Binding
CHEMBL4375085
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of N-terminal fluorescein labelled Puma-BH3 peptide from human N-terminal thrombin cleavage site-fused/His6-tagged Bcl-2 expressed in Escherichia coliBL21(DE3) pLysS cells by fluorescence polarization assay
23
Total Activities
22
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-Guided Discovery of a Selective Mcl-1 Inhibitor with Cellular Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 4.78 | 5.89 |
| IC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4521569 | — | — | 1 | 5.89 |
| CHEMBL4472592 | — | — | 1 | 5.39 |
| CHEMBL4521112 | — | — | 1 | 5.30 |
| CHEMBL4464302 | — | — | 1 | 5.27 |
| CHEMBL4467044 | — | — | 1 | 5.21 |
| CHEMBL4455822 | — | — | 1 | 5.09 |
| CHEMBL4460382 | — | — | 1 | 4.89 |
| CHEMBL4524567 | — | — | 1 | 4.68 |
| CHEMBL4514111 | — | — | 1 | 4.62 |
| CHEMBL4450255 | — | — | 1 | 4.62 |
| CHEMBL4450405 | — | — | 1 | 4.55 |
| CHEMBL4515659 | — | — | 1 | 4.54 |
| CHEMBL4452148 | — | — | 1 | 4.44 |
| CHEMBL4443675 | — | — | 1 | 4.31 |
| CHEMBL4442085 | — | — | 1 | 4.29 |
| CHEMBL4572199 | — | — | 2 | 4.13 |
| CHEMBL4573285 | — | — | 1 | 4.01 |
| CHEMBL4458787 | — | — | 1 | - |
| CHEMBL4455139 | — | — | 1 | - |
| CHEMBL4471326 | — | — | 1 | - |
| CHEMBL4440978 | — | — | 1 | - |
| CHEMBL4460632 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4521569 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL4472592 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL4521112 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL4464302 | — | Ki | = | 5400.0 | nM | 5.27 |
| CHEMBL4467044 | — | Ki | = | 6100.0 | nM | 5.21 |
| CHEMBL4455822 | — | Ki | = | 8100.0 | nM | 5.09 |
| CHEMBL4460382 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL4524567 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL4514111 | — | Ki | = | 24000.0 | nM | 4.62 |
| CHEMBL4450255 | — | Ki | = | 24000.0 | nM | 4.62 |
| CHEMBL4450405 | — | Ki | = | 28000.0 | nM | 4.55 |
| CHEMBL4515659 | — | Ki | = | 29000.0 | nM | 4.54 |
| CHEMBL4452148 | — | Ki | = | 36000.0 | nM | 4.44 |
| CHEMBL4443675 | — | Ki | = | 49000.0 | nM | 4.31 |
| CHEMBL4442085 | — | Ki | = | 51000.0 | nM | 4.29 |
| CHEMBL4572199 | — | Ki | = | 74000.0 | nM | 4.13 |
| CHEMBL4573285 | — | Ki | = | 98000.0 | nM | 4.01 |
| CHEMBL4572199 | — | IC50 | = | 164000.0 | nM | - |
| CHEMBL4458787 | — | Ki | = | 418000.0 | nM | - |
| CHEMBL4440978 | — | Ki | = | 359000.0 | nM | - |
| CHEMBL4455139 | — | Ki | = | 470000.0 | nM | - |
| CHEMBL4471326 | — | Ki | = | 269000.0 | nM | - |
| CHEMBL4460632 | — | Ki | = | 437000.0 | nM | - |