Assay Detail
Binding
CHEMBL4375084
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of N-terminal fluorescein labelled Puma-BH3 peptide from TEV-fused His-tagged human Mcl-1 expressed in Escherichia coliBL21(DE3) pLysS cells after 2 hrs by fluorescence polarization assay
55
Total Activities
47
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
Structure-Guided Discovery of a Selective Mcl-1 Inhibitor with Cellular Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 55 | 5.30 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4472351 | — | — | 2 | 7.72 |
| CHEMBL4465591 | — | — | 1 | 7.68 |
| CHEMBL4450734 | — | — | 1 | 7.50 |
| CHEMBL4537357 | — | — | 1 | 7.34 |
| CHEMBL4515048 | — | — | 1 | 7.29 |
| CHEMBL4573959 | — | — | 1 | 7.12 |
| CHEMBL4451346 | — | — | 2 | 6.66 |
| CHEMBL4437381 | — | — | 1 | 6.58 |
| CHEMBL4443008 | — | — | 2 | 6.48 |
| CHEMBL4456457 | — | — | 2 | 6.31 |
| CHEMBL4515659 | — | — | 1 | 6.29 |
| CHEMBL4452148 | — | — | 1 | 6.09 |
| CHEMBL4473708 | — | — | 2 | 6.05 |
| CHEMBL4436725 | — | — | 2 | 5.80 |
| CHEMBL4452383 | — | — | 1 | 5.70 |
| CHEMBL4458675 | — | — | 2 | 5.62 |
| CHEMBL4529278 | — | — | 1 | 5.55 |
| CHEMBL4445863 | — | — | 1 | 5.22 |
| CHEMBL4455139 | — | — | 1 | 5.11 |
| CHEMBL4448750 | — | — | 1 | 5.09 |
| CHEMBL4472592 | — | — | 1 | 5.08 |
| CHEMBL4580279 | — | — | 1 | 5.00 |
| CHEMBL4476787 | — | — | 2 | 4.82 |
| CHEMBL4467044 | — | — | 1 | 4.72 |
| CHEMBL4464302 | — | — | 1 | 4.72 |
| CHEMBL4460632 | — | — | 1 | 4.68 |
| CHEMBL4450405 | — | — | 1 | 4.66 |
| CHEMBL4547333 | — | — | 1 | 4.62 |
| CHEMBL4524567 | — | — | 1 | 4.62 |
| CHEMBL4443675 | — | — | 1 | 4.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4472351 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4465591 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4450734 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL4537357 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL4515048 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL4573959 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL4451346 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL4437381 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL4443008 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL4456457 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL4515659 | — | Ki | = | 510.0 | nM | 6.29 |
| CHEMBL4456457 | — | Ki | = | 640.0 | nM | 6.19 |
| CHEMBL4452148 | — | Ki | = | 810.0 | nM | 6.09 |
| CHEMBL4473708 | — | Ki | = | 890.0 | nM | 6.05 |
| CHEMBL4436725 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL4452383 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL4458675 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL4529278 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL4473708 | — | Ki | = | 3400.0 | nM | 5.47 |
| CHEMBL4443008 | — | Ki | = | 5300.0 | nM | 5.28 |
| CHEMBL4436725 | — | Ki | = | 5700.0 | nM | 5.24 |
| CHEMBL4445863 | — | Ki | = | 6000.0 | nM | 5.22 |
| CHEMBL4455139 | — | Ki | = | 7700.0 | nM | 5.11 |
| CHEMBL4448750 | — | Ki | = | 8100.0 | nM | 5.09 |
| CHEMBL4472592 | — | Ki | = | 8400.0 | nM | 5.08 |
| CHEMBL4580279 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL4476787 | — | Ki | = | 15000.0 | nM | 4.82 |
| CHEMBL4476787 | — | Ki | = | 18000.0 | nM | 4.75 |
| CHEMBL4464302 | — | Ki | = | 19000.0 | nM | 4.72 |
| CHEMBL4467044 | — | Ki | = | 19000.0 | nM | 4.72 |
| CHEMBL4460632 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL4450405 | — | Ki | = | 22000.0 | nM | 4.66 |
| CHEMBL4547333 | — | Ki | = | 24000.0 | nM | 4.62 |
| CHEMBL4524567 | — | Ki | = | 24000.0 | nM | 4.62 |
| CHEMBL4472351 | — | Ki | = | 25000.0 | nM | 4.60 |
| CHEMBL4443675 | — | Ki | = | 27000.0 | nM | 4.57 |
| CHEMBL4471326 | — | Ki | = | 27000.0 | nM | 4.57 |
| CHEMBL4440978 | — | Ki | = | 44000.0 | nM | 4.36 |
| CHEMBL4442085 | — | Ki | = | 44000.0 | nM | 4.36 |
| CHEMBL4521112 | — | Ki | = | 45000.0 | nM | 4.35 |
| CHEMBL4572199 | — | Ki | = | 50000.0 | nM | 4.30 |
| CHEMBL4521569 | — | Ki | = | 50000.0 | nM | 4.30 |
| CHEMBL4514111 | — | Ki | = | 51000.0 | nM | 4.29 |
| CHEMBL4455822 | — | Ki | = | 53000.0 | nM | 4.28 |
| CHEMBL4516603 | — | Ki | = | 58000.0 | nM | 4.24 |
| CHEMBL4458675 | — | Ki | = | 58000.0 | nM | 4.24 |
| CHEMBL4448439 | — | Ki | = | 59000.0 | nM | 4.23 |
| CHEMBL4456249 | — | Ki | = | 61000.0 | nM | 4.21 |
| CHEMBL4460382 | — | Ki | = | 68000.0 | nM | 4.17 |
| CHEMBL4450255 | — | Ki | = | 77000.0 | nM | 4.11 |