Assay Detail
Binding
CHEMBL3783777
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His6-MBP tagged recombinant human Mcl-1 residues 172 to 327 expressed in Escherichia coli assessed as inhibition of interaction with Bak BH3 peptide (GQVGRQLAIIGDDINR) after 3 hrs by fluorescence polarization competition assay
48
Total Activities
48
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 |
Target
Induced myeloid leukemia cell differentiation protein Mcl-1 (CHEMBL4361) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-based design of N-substituted 1-hydroxy-4-sulfamoyl-2-naphthoates as selective inhibitors of the Mcl-1 oncoprotein.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 46 | 5.61 | 7.51 |
| Inhibition | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3781822 | — | — | 1 | 7.51 |
| CHEMBL3780397 | — | — | 1 | 7.48 |
| CHEMBL3780803 | — | — | 1 | 7.10 |
| CHEMBL3781669 | — | — | 1 | 7.10 |
| CHEMBL3780225 | — | — | 1 | 7.09 |
| CHEMBL3780311 | — | — | 1 | 6.94 |
| CHEMBL3780473 | — | — | 1 | 6.93 |
| CHEMBL3780719 | — | — | 1 | 6.76 |
| CHEMBL3781894 | — | — | 1 | 6.55 |
| CHEMBL3781396 | — | — | 1 | 6.47 |
| CHEMBL3780113 | — | — | 1 | 6.38 |
| CHEMBL3780576 | — | — | 1 | 6.31 |
| CHEMBL3781019 | — | — | 1 | 6.25 |
| CHEMBL3781946 | — | — | 1 | 5.94 |
| CHEMBL3780617 | — | — | 1 | 5.81 |
| CHEMBL3780990 | — | — | 1 | 5.73 |
| CHEMBL3780290 | — | — | 1 | 5.72 |
| CHEMBL3781065 | — | — | 1 | 5.60 |
| CHEMBL3781059 | — | — | 1 | 5.56 |
| CHEMBL3780988 | — | — | 1 | 5.53 |
| CHEMBL3781593 | — | — | 1 | 5.47 |
| CHEMBL3781692 | — | — | 1 | 5.41 |
| CHEMBL3781823 | — | — | 1 | 5.39 |
| CHEMBL3781264 | — | — | 1 | 5.35 |
| CHEMBL3781502 | — | — | 1 | 5.34 |
| CHEMBL3780385 | — | — | 1 | 5.34 |
| CHEMBL3781868 | — | — | 1 | 5.30 |
| CHEMBL3780899 | — | — | 1 | 5.25 |
| CHEMBL3781478 | — | — | 1 | 5.17 |
| CHEMBL3780058 | — | — | 1 | 5.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3781822 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL3780397 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL3781669 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL3780803 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL3780225 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL3780311 | — | Ki | = | 114.0 | nM | 6.94 |
| CHEMBL3780473 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL3780719 | — | Ki | = | 173.0 | nM | 6.76 |
| CHEMBL3781894 | — | Ki | = | 284.0 | nM | 6.55 |
| CHEMBL3781396 | — | Ki | = | 335.0 | nM | 6.47 |
| CHEMBL3780113 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL3780576 | — | Ki | = | 487.0 | nM | 6.31 |
| CHEMBL3781019 | — | Ki | = | 566.0 | nM | 6.25 |
| CHEMBL3781946 | — | Ki | = | 1150.0 | nM | 5.94 |
| CHEMBL3780617 | — | Ki | = | 1540.0 | nM | 5.81 |
| CHEMBL3780990 | — | Ki | = | 1880.0 | nM | 5.73 |
| CHEMBL3780290 | — | Ki | = | 1910.0 | nM | 5.72 |
| CHEMBL3781065 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL3781059 | — | Ki | = | 2760.0 | nM | 5.56 |
| CHEMBL3780988 | — | Ki | = | 2950.0 | nM | 5.53 |
| CHEMBL3781593 | — | Ki | = | 3410.0 | nM | 5.47 |
| CHEMBL3781692 | — | Ki | = | 3860.0 | nM | 5.41 |
| CHEMBL3781823 | — | Ki | = | 4050.0 | nM | 5.39 |
| CHEMBL3781264 | — | Ki | = | 4490.0 | nM | 5.35 |
| CHEMBL3781502 | — | Ki | = | 4580.0 | nM | 5.34 |
| CHEMBL3780385 | — | Ki | = | 4540.0 | nM | 5.34 |
| CHEMBL3781868 | — | Ki | = | 5030.0 | nM | 5.30 |
| CHEMBL3780899 | — | Ki | = | 5640.0 | nM | 5.25 |
| CHEMBL3781478 | — | Ki | = | 6840.0 | nM | 5.17 |
| CHEMBL3780058 | — | Ki | = | 7310.0 | nM | 5.14 |
| CHEMBL3780451 | — | Ki | = | 8500.0 | nM | 5.07 |
| CHEMBL3780357 | — | Ki | = | 11200.0 | nM | 4.95 |
| CHEMBL3780070 | — | Ki | = | 11900.0 | nM | 4.92 |
| CHEMBL3780331 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL3780766 | — | Ki | = | 22200.0 | nM | 4.65 |
| CHEMBL3779915 | — | Ki | = | 23400.0 | nM | 4.63 |
| CHEMBL3780614 | — | Ki | = | 25700.0 | nM | 4.59 |
| CHEMBL3780382 | — | Ki | = | 26900.0 | nM | 4.57 |
| CHEMBL3780094 | — | Ki | = | 34300.0 | nM | 4.46 |
| CHEMBL3781306 | — | Ki | = | 50300.0 | nM | 4.30 |
| CHEMBL3780580 | — | Ki | = | 54000.0 | nM | 4.27 |
| CHEMBL3780355 | — | Ki | = | 56300.0 | nM | 4.25 |
| CHEMBL1410420 | — | Ki | = | 99000.0 | nM | 4.00 |
| CHEMBL3780242 | — | Ki | > | 500000.0 | nM | - |
| CHEMBL3781985 | — | Ki | > | 500000.0 | nM | - |
| CHEMBL3780724 | — | Ki | = | 106000.0 | nM | - |
| CHEMBL3781188 | — | Inhibition | - | % | - | |
| CHEMBL3780087 | — | Inhibition | - | % | - |