Assay Detail
Binding
CHEMBL1019892
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Inhibition of GST fused Bcl-2 binding to biotinylated 16 mer Bak-BH3 peptide by HTRF-LANCE assay
35
Total Activities
35
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Tetrahydroisoquinoline amide substituted phenyl pyrazoles as selective Bcl-2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 6.44 | 8.00 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL473446 | — | — | 1 | 8.00 |
| CHEMBL509208 | — | — | 1 | 7.70 |
| CHEMBL481581 | — | — | 1 | 7.70 |
| CHEMBL503454 | — | — | 1 | 7.52 |
| CHEMBL504480 | — | — | 1 | 7.40 |
| CHEMBL449546 | — | — | 1 | 7.40 |
| CHEMBL509788 | — | — | 1 | 7.40 |
| CHEMBL460173 | — | — | 1 | 7.30 |
| CHEMBL481775 | — | — | 1 | 7.05 |
| CHEMBL467229 | — | — | 1 | 7.00 |
| CHEMBL514298 | — | — | 1 | 6.96 |
| CHEMBL453380 | — | — | 1 | 6.96 |
| CHEMBL500866 | — | — | 1 | 6.85 |
| CHEMBL500574 | — | — | 1 | 6.82 |
| CHEMBL501871 | — | — | 1 | 6.80 |
| CHEMBL444140 | — | — | 1 | 6.72 |
| CHEMBL513318 | — | — | 1 | 6.64 |
| CHEMBL450954 | — | — | 1 | 6.60 |
| CHEMBL453466 | — | — | 1 | 6.55 |
| CHEMBL510332 | — | — | 1 | 6.14 |
| CHEMBL517577 | — | — | 1 | 6.10 |
| CHEMBL446802 | — | — | 1 | 6.09 |
| CHEMBL446607 | — | — | 1 | 5.98 |
| CHEMBL516633 | — | — | 1 | 5.85 |
| CHEMBL464268 | — | — | 1 | 5.82 |
| CHEMBL480009 | — | — | 1 | 5.72 |
| CHEMBL518858 | — | — | 1 | 5.64 |
| CHEMBL466801 | — | — | 1 | 5.60 |
| CHEMBL480008 | — | — | 1 | 5.52 |
| CHEMBL520607 | — | — | 1 | 5.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL473446 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL509208 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL481581 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL503454 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL504480 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL449546 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL509788 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL460173 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL481775 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL467229 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL514298 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL453380 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL500866 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL500574 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL501871 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL444140 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL513318 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL450954 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL453466 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL510332 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL517577 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL446802 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL446607 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL516633 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL464268 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL480009 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL518858 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL466801 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL480008 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL520607 | — | IC50 | = | 3670.0 | nM | 5.43 |
| CHEMBL446480 | — | IC50 | = | 5610.0 | nM | 5.25 |
| CHEMBL480010 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL469305 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL464440 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL466802 | — | Activity | - | — | - |