Assay Detail
Binding
CHEMBL4344314
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His6-tagged human Bfl-1 (1 to 151 residues), expressed in Escherichia coli Rosetta2 DE3 by fluorescent labeled FAM-Bid peptide based fluorescence polarization assay
27
Total Activities
27
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
Discovery and Characterization of 2,5-Substituted Benzoic Acid Dual Inhibitors of the Anti-apoptotic Mcl-1 and Bfl-1 Proteins.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 5.98 | 7.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4522193 | — | — | 1 | 7.08 |
| CHEMBL4533559 | — | — | 1 | 7.00 |
| CHEMBL4576854 | — | — | 1 | 7.00 |
| CHEMBL4558313 | — | — | 1 | 6.82 |
| CHEMBL4462138 | — | — | 1 | 6.77 |
| CHEMBL4454113 | — | — | 1 | 6.60 |
| CHEMBL4463305 | — | — | 1 | 6.55 |
| CHEMBL4452560 | — | — | 1 | 6.41 |
| CHEMBL4457901 | — | — | 1 | 6.24 |
| CHEMBL4475729 | — | — | 1 | 6.12 |
| CHEMBL4435041 | — | — | 1 | 6.09 |
| CHEMBL4440719 | — | — | 1 | 6.05 |
| CHEMBL4473975 | — | — | 1 | 6.00 |
| CHEMBL4525910 | — | — | 1 | 5.96 |
| CHEMBL4448621 | — | — | 1 | 5.80 |
| CHEMBL4577267 | — | — | 1 | 5.77 |
| CHEMBL4461974 | — | — | 1 | 5.52 |
| CHEMBL4463594 | — | — | 1 | 5.47 |
| CHEMBL4442233 | — | — | 1 | 5.43 |
| CHEMBL4459843 | — | — | 1 | 5.42 |
| CHEMBL4435893 | — | — | 1 | 5.34 |
| CHEMBL4528399 | — | — | 1 | 4.97 |
| CHEMBL4534654 | — | — | 1 | 4.83 |
| CHEMBL4553113 | — | — | 1 | 4.21 |
| CHEMBL4461424 | — | — | 1 | - |
| CHEMBL4456253 | — | — | 1 | - |
| CHEMBL285503 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4522193 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL4533559 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4576854 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4558313 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL4462138 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL4454113 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL4463305 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL4452560 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL4457901 | — | Ki | = | 570.0 | nM | 6.24 |
| CHEMBL4475729 | — | Ki | = | 760.0 | nM | 6.12 |
| CHEMBL4435041 | — | Ki | = | 810.0 | nM | 6.09 |
| CHEMBL4440719 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL4473975 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL4525910 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL4448621 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL4577267 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL4461974 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL4463594 | — | Ki | = | 3400.0 | nM | 5.47 |
| CHEMBL4442233 | — | Ki | = | 3700.0 | nM | 5.43 |
| CHEMBL4459843 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL4435893 | — | Ki | = | 4600.0 | nM | 5.34 |
| CHEMBL4528399 | — | Ki | = | 10600.0 | nM | 4.97 |
| CHEMBL4534654 | — | Ki | = | 14800.0 | nM | 4.83 |
| CHEMBL4553113 | — | Ki | = | 62000.0 | nM | 4.21 |
| CHEMBL4461424 | — | Ki | > | 70000.0 | nM | - |
| CHEMBL4456253 | — | Ki | > | 70000.0 | nM | - |
| CHEMBL285503 | — | Ki | > | 100000.0 | nM | - |