Assay Detail
ADMET
CHEMBL4730613
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Inhibition of F-Bak (GQVGRQLAIIGDK(6-FAM)INR-amide) F-Bak(GQVGRQLAIIGDK(6-FAM)INR-amide) binding to BCL2 (unknown origin) incubated for 1 hr by TR-FRET assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.90 | 8.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3793424 | — | — | 1 | 8.21 |
| CHEMBL3919588 | — | — | 1 | 7.54 |
| CHEMBL3935328 | — | — | 1 | 7.16 |
| CHEMBL3972984 | — | — | 1 | 6.93 |
| CHEMBL3901568 | — | — | 1 | 6.92 |
| CHEMBL3983880 | — | — | 1 | 6.46 |
| CHEMBL3912857 | — | — | 1 | 6.38 |
| CHEMBL3891330 | — | — | 1 | 6.26 |
| CHEMBL3287296 | — | — | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3793424 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL3919588 | — | Ki | = | 28.5 | nM | 7.54 |
| CHEMBL3935328 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL3972984 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL3901568 | — | Ki | = | 119.0 | nM | 6.92 |
| CHEMBL3983880 | — | Ki | = | 348.0 | nM | 6.46 |
| CHEMBL3912857 | — | Ki | = | 413.0 | nM | 6.38 |
| CHEMBL3891330 | — | Ki | = | 548.0 | nM | 6.26 |
| CHEMBL3287296 | — | Ki | = | 626.0 | nM | 6.20 |