Assay Detail
Binding
CHEMBL5034987
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Binding affinity to full length human Bcl-2 expressed in Escherichia coli BL21 (DE3) assessed as inhibition constant preincubated for 30 mins followed by 5-FAM-QEDIIIINIARHLAQVGDSMD-RSIPPG tracer addition and measured after 20 mins by fluorescence polarization assay
13
Total Activities
13
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
Structure-Based Optimization of 3-Phenyl-<i>N</i>-(2-(3-phenylureido)ethyl)thiophene-2-sulfonamide Derivatives as Selective Mcl-1 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 5.30 | 5.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5092439 | — | — | 1 | 5.62 |
| CHEMBL5091070 | — | — | 1 | 5.58 |
| CHEMBL5088505 | — | — | 1 | 5.54 |
| CHEMBL5079843 | — | — | 1 | 5.44 |
| CHEMBL5079372 | — | — | 1 | 5.41 |
| CHEMBL5078508 | — | — | 1 | 5.34 |
| CHEMBL5089281 | — | — | 1 | 5.34 |
| CHEMBL5080325 | — | — | 1 | 5.28 |
| CHEMBL5076953 | — | — | 1 | 5.25 |
| CHEMBL5078562 | — | — | 1 | 5.08 |
| CHEMBL5083087 | — | — | 1 | 4.89 |
| CHEMBL5090868 | — | — | 1 | 4.77 |
| CHEMBL3137309 | VENETOCLAX | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5092439 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL5091070 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL5088505 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL5079843 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL5079372 | — | Ki | = | 3900.0 | nM | 5.41 |
| CHEMBL5078508 | — | Ki | = | 4600.0 | nM | 5.34 |
| CHEMBL5089281 | — | Ki | = | 4600.0 | nM | 5.34 |
| CHEMBL5080325 | — | Ki | = | 5200.0 | nM | 5.28 |
| CHEMBL5076953 | — | Ki | = | 5600.0 | nM | 5.25 |
| CHEMBL5078562 | — | Ki | = | 8400.0 | nM | 5.08 |
| CHEMBL5083087 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL5090868 | — | Ki | = | 17000.0 | nM | 4.77 |
| CHEMBL3137309 | VENETOCLAX | Ki | < | 1.0 | nM | - |