Assay Detail
Binding
CHEMBL3375466
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BTK (unknown origin) using biotin-labeled peptide substrate incubated for 1 hr by TR-FRET based HTRF kinase assay
19
Total Activities
19
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 |
Publication
Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.88 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3358397 | — | — | 1 | 8.05 |
| CHEMBL2057918 | — | — | 1 | 7.89 |
| CHEMBL3358396 | — | — | 1 | 7.80 |
| CHEMBL3358395 | — | — | 1 | 7.70 |
| CHEMBL3358398 | — | — | 1 | 7.55 |
| CHEMBL3358399 | — | — | 1 | 7.43 |
| CHEMBL3358408 | — | — | 1 | 6.69 |
| CHEMBL3358401 | — | — | 1 | 6.59 |
| CHEMBL3358407 | — | — | 1 | 6.44 |
| CHEMBL3358402 | — | — | 1 | 6.37 |
| CHEMBL3358406 | — | — | 1 | 6.30 |
| CHEMBL3358400 | — | — | 1 | 6.25 |
| CHEMBL3358405 | — | — | 1 | 6.09 |
| CHEMBL3358409 | — | — | 1 | 6.06 |
| CHEMBL3358403 | — | — | 1 | 5.99 |
| CHEMBL3358412 | — | — | 1 | - |
| CHEMBL3358404 | — | — | 1 | - |
| CHEMBL3358410 | — | — | 1 | - |
| CHEMBL3358411 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3358397 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2057918 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3358396 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3358395 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3358398 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3358399 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3358408 | — | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL3358401 | — | IC50 | = | 255.0 | nM | 6.59 |
| CHEMBL3358407 | — | IC50 | = | 365.0 | nM | 6.44 |
| CHEMBL3358402 | — | IC50 | = | 431.0 | nM | 6.37 |
| CHEMBL3358406 | — | IC50 | = | 503.0 | nM | 6.30 |
| CHEMBL3358400 | — | IC50 | = | 564.0 | nM | 6.25 |
| CHEMBL3358405 | — | IC50 | = | 818.0 | nM | 6.09 |
| CHEMBL3358409 | — | IC50 | = | 875.0 | nM | 6.06 |
| CHEMBL3358403 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL3358412 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL3358404 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL3358410 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL3358411 | — | IC50 | > | 5000.0 | nM | - |