Assay Detail
Binding
CHEMBL5124386
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BTK C481S mutant (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 30 mins in presence of ATP by Microfluidic chip based mobility shift assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Medicinal Chemistry Strategies for the Development of Bruton's Tyrosine Kinase Inhibitors against Resistance.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.68 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5169992 | — | — | 1 | 8.60 |
| CHEMBL5177238 | — | — | 1 | 8.52 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 8.34 |
| CHEMBL5197089 | — | — | 1 | 8.33 |
| CHEMBL5187230 | — | — | 1 | 8.28 |
| CHEMBL5206888 | — | — | 1 | 8.20 |
| CHEMBL5195945 | — | — | 1 | 8.13 |
| CHEMBL5195670 | — | — | 1 | 6.76 |
| CHEMBL5201319 | — | — | 1 | 6.72 |
| CHEMBL5198054 | — | — | 1 | 6.61 |
| CHEMBL3301625 | SPEBRUTINIB | 2.0 | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5169992 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5177238 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL5197089 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL5187230 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL5206888 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL5195945 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL5195670 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL5201319 | — | IC50 | = | 191.0 | nM | 6.72 |
| CHEMBL5198054 | — | IC50 | = | 247.0 | nM | 6.61 |
| CHEMBL3301625 | SPEBRUTINIB | IC50 | = | 908.0 | nM | 6.04 |