Assay Detail
Binding
CHEMBL3375467
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BTK in human Ramos cells assessed as reduction in IgM-induced calcium influx incubated for 20 mins by Fluo-4 dye based fluorescence assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Ramos |
| 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 | 6.77 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3358396 | — | — | 1 | 8.10 |
| CHEMBL3358395 | — | — | 1 | 7.68 |
| CHEMBL2057918 | — | — | 1 | 7.57 |
| CHEMBL3358397 | — | — | 1 | 7.48 |
| CHEMBL3358399 | — | — | 1 | 6.94 |
| CHEMBL3358401 | — | — | 1 | 6.91 |
| CHEMBL3358408 | — | — | 1 | 6.77 |
| CHEMBL3358407 | — | — | 1 | 6.59 |
| CHEMBL3358406 | — | — | 1 | 6.33 |
| CHEMBL3358402 | — | — | 1 | 5.99 |
| CHEMBL3358400 | — | — | 1 | 5.49 |
| CHEMBL3358398 | — | — | 1 | 5.36 |
| CHEMBL3358412 | — | — | 1 | - |
| CHEMBL3358410 | — | — | 1 | - |
| CHEMBL3358411 | — | — | 1 | - |
| CHEMBL3358403 | — | — | 1 | - |
| CHEMBL3358404 | — | — | 1 | - |
| CHEMBL3358405 | — | — | 1 | - |
| CHEMBL3358409 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3358396 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3358395 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2057918 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3358397 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3358399 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL3358401 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL3358408 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL3358407 | — | IC50 | = | 254.0 | nM | 6.59 |
| CHEMBL3358406 | — | IC50 | = | 472.0 | nM | 6.33 |
| CHEMBL3358402 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL3358400 | — | IC50 | = | 3250.0 | nM | 5.49 |
| CHEMBL3358398 | — | IC50 | = | 4360.0 | nM | 5.36 |
| CHEMBL3358412 | — | IC50 | - | — | - | |
| CHEMBL3358410 | — | IC50 | - | — | - | |
| CHEMBL3358411 | — | IC50 | - | — | - | |
| CHEMBL3358403 | — | IC50 | - | — | - | |
| CHEMBL3358404 | — | IC50 | - | — | - | |
| CHEMBL3358405 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL3358409 | — | IC50 | > | 5000.0 | nM | - |