Assay Detail
Functional
CHEMBL985387
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Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl2 assessed as cell viability after 24 hrs by MTS assay in absence of serum
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | FL5.12 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 17 | 7.51 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL448740 | — | — | 1 | 9.22 |
| CHEMBL508865 | — | — | 1 | 8.96 |
| CHEMBL501889 | — | — | 1 | 8.33 |
| CHEMBL443684 | NAVITOCLAX | 3.0 | 1 | 8.23 |
| CHEMBL376408 | ABT 737 | 1.0 | 1 | 8.11 |
| CHEMBL466090 | — | — | 1 | 7.96 |
| CHEMBL452892 | — | — | 1 | 7.48 |
| CHEMBL473870 | — | — | 1 | 7.41 |
| CHEMBL510351 | — | — | 1 | 7.38 |
| CHEMBL444481 | — | — | 1 | 7.31 |
| CHEMBL469778 | — | — | 1 | 7.29 |
| CHEMBL510761 | — | — | 1 | 7.26 |
| CHEMBL508210 | — | — | 1 | 6.77 |
| CHEMBL449676 | — | — | 1 | 6.64 |
| CHEMBL509460 | — | — | 1 | 6.17 |
| CHEMBL508864 | — | — | 1 | 5.57 |
| CHEMBL451683 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL448740 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL508865 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL501889 | — | EC50 | = | 4.7 | nM | 8.33 |
| CHEMBL443684 | NAVITOCLAX | EC50 | = | 5.9 | nM | 8.23 |
| CHEMBL376408 | ABT 737 | EC50 | = | 7.7 | nM | 8.11 |
| CHEMBL466090 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL452892 | — | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL473870 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL510351 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL444481 | — | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL469778 | — | EC50 | = | 51.0 | nM | 7.29 |
| CHEMBL510761 | — | EC50 | = | 55.0 | nM | 7.26 |
| CHEMBL508210 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL449676 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL509460 | — | EC50 | = | 673.0 | nM | 6.17 |
| CHEMBL508864 | — | EC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL451683 | — | EC50 | < | 1.0 | nM | - |