Assay Detail
Binding
CHEMBL5363740
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of Cy5-labeled BIM BH3 peptide (H3N-(C/Cy5Mal)-WIAQELRRIGDEFN-OH) from MCL-1 (unknown origin) assessed as inhibition constant incubated for 60 mins by HTRF assay
14
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 |
Target
Induced myeloid leukemia cell differentiation protein Mcl-1 (CHEMBL4361) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Macrocyclic Carbon-Linked Pyrazoles As Novel Inhibitors of MCL-1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 10.38 | 10.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5396628 | — | — | 1 | 10.89 |
| CHEMBL5307201 | — | — | 1 | 10.82 |
| CHEMBL5400376 | — | — | 1 | 10.74 |
| CHEMBL5402764 | — | — | 1 | 10.70 |
| CHEMBL5426737 | — | — | 1 | 10.70 |
| CHEMBL5437853 | — | — | 1 | 10.66 |
| CHEMBL5412641 | — | — | 1 | 10.64 |
| CHEMBL5394656 | — | — | 1 | 10.49 |
| CHEMBL5437622 | — | — | 1 | 10.47 |
| CHEMBL5433387 | — | — | 1 | 10.40 |
| CHEMBL5405517 | — | — | 1 | 10.39 |
| CHEMBL5402950 | — | — | 1 | 10.33 |
| CHEMBL5403706 | — | — | 2 | 10.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5396628 | — | Ki | = | 0.013 | nM | 10.89 |
| CHEMBL5307201 | — | Ki | = | 0.015 | nM | 10.82 |
| CHEMBL5400376 | — | Ki | = | 0.018 | nM | 10.74 |
| CHEMBL5402764 | — | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL5426737 | — | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL5437853 | — | Ki | = | 0.022 | nM | 10.66 |
| CHEMBL5412641 | — | Ki | = | 0.023 | nM | 10.64 |
| CHEMBL5394656 | — | Ki | = | 0.032 | nM | 10.49 |
| CHEMBL5437622 | — | Ki | = | 0.034 | nM | 10.47 |
| CHEMBL5433387 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL5405517 | — | Ki | = | 0.041 | nM | 10.39 |
| CHEMBL5402950 | — | Ki | = | 0.047 | nM | 10.33 |
| CHEMBL5403706 | — | Ki | = | 0.069 | nM | 10.16 |
| CHEMBL5403706 | — | Ki | = | 11.0 | nM | 7.96 |