Assay Detail
Binding
CHEMBL4356586
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant C-terminal His6x-tagged human Mcl-1 (171 to 327 residues) interaction with biotinylated human Bim (51 to 76 residues) incubated for 60 mins in presence of 0.05 nM biotin-Bim by HTRF assay
29
Total Activities
29
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
Discovery and in Vivo Evaluation of Macrocyclic Mcl-1 Inhibitors Featuring an α-Hydroxy Phenylacetic Acid Pharmacophore or Bioisostere.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 8.72 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4553660 | — | — | 1 | 9.70 |
| CHEMBL4535151 | — | — | 1 | 9.70 |
| CHEMBL4580244 | — | — | 1 | 9.70 |
| CHEMBL4464768 | — | — | 1 | 9.52 |
| CHEMBL4539543 | — | — | 1 | 9.52 |
| CHEMBL4446369 | — | — | 1 | 9.52 |
| CHEMBL4528051 | — | — | 1 | 9.52 |
| CHEMBL4446378 | TAPOTOCLAX | 1.0 | 1 | 9.52 |
| CHEMBL4438074 | — | — | 1 | 9.40 |
| CHEMBL4588330 | — | — | 1 | 9.30 |
| CHEMBL4437832 | — | — | 1 | 9.30 |
| CHEMBL4577379 | — | — | 1 | 9.30 |
| CHEMBL4547370 | — | — | 1 | 9.22 |
| CHEMBL4542646 | — | — | 1 | 9.22 |
| CHEMBL4593361 | — | — | 1 | 9.13 |
| CHEMBL4562159 | — | — | 1 | 9.00 |
| CHEMBL4452794 | — | — | 1 | 8.96 |
| CHEMBL4469850 | — | — | 1 | 8.89 |
| CHEMBL4561691 | — | — | 1 | 8.77 |
| CHEMBL4452403 | — | — | 1 | 8.30 |
| CHEMBL4446955 | — | — | 1 | 8.00 |
| CHEMBL4544042 | — | — | 1 | 8.00 |
| CHEMBL4460664 | — | — | 1 | 7.96 |
| CHEMBL4522764 | — | — | 1 | 7.82 |
| CHEMBL4515030 | — | — | 1 | 7.57 |
| CHEMBL4452437 | — | — | 1 | 7.46 |
| CHEMBL4574884 | — | — | 1 | 7.08 |
| CHEMBL4463461 | — | — | 1 | 6.82 |
| CHEMBL4543603 | — | — | 1 | 6.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4553660 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4535151 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4580244 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4464768 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4539543 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4446369 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4528051 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4446378 | TAPOTOCLAX | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4438074 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4588330 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4437832 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4577379 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4547370 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4542646 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4593361 | — | IC50 | = | 0.74 | nM | 9.13 |
| CHEMBL4562159 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4452794 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4469850 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4561691 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4452403 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4446955 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4544042 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4460664 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4522764 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4515030 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4452437 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4574884 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4463461 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL4543603 | — | IC50 | = | 281.0 | nM | 6.55 |