Assay Detail
Functional
CHEMBL5349014
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Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | MV4-11 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
From PROTAC to inhibitor: Structure-guided discovery of potent and orally bioavailable BET inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.90 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5440963 | — | — | 1 | 7.75 |
| CHEMBL5432745 | — | — | 1 | 7.70 |
| CHEMBL3581647 | BIRABRESIB | 2.0 | 1 | 7.66 |
| CHEMBL5440537 | — | — | 1 | 7.50 |
| CHEMBL5400310 | — | — | 1 | 7.48 |
| CHEMBL5439607 | — | — | 1 | 7.40 |
| CHEMBL5420752 | — | — | 1 | 7.23 |
| CHEMBL1957266 | — | — | 1 | 7.00 |
| CHEMBL5403848 | — | — | 1 | 6.84 |
| CHEMBL5398000 | — | — | 1 | 6.74 |
| CHEMBL5422163 | — | — | 1 | 6.60 |
| CHEMBL5424952 | — | — | 1 | 6.53 |
| CHEMBL5436475 | — | — | 1 | 6.35 |
| CHEMBL5401253 | — | — | 1 | 6.14 |
| CHEMBL5399489 | — | — | 1 | 5.94 |
| CHEMBL5422881 | — | — | 1 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5440963 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5432745 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3581647 | BIRABRESIB | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5440537 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5400310 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5439607 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5420752 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL1957266 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL5403848 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL5398000 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL5422163 | — | IC50 | = | 253.0 | nM | 6.60 |
| CHEMBL5424952 | — | IC50 | = | 297.0 | nM | 6.53 |
| CHEMBL5436475 | — | IC50 | = | 444.0 | nM | 6.35 |
| CHEMBL5401253 | — | IC50 | = | 729.0 | nM | 6.14 |
| CHEMBL5399489 | — | IC50 | = | 1138.0 | nM | 5.94 |
| CHEMBL5422881 | — | IC50 | = | 3055.0 | nM | 5.51 |