Assay Detail
Binding
CHEMBL5124385
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His-tagged full-length recombinant wild-type human BTK (Ala2 to Ser659 residues) expressed in baculovirus infected 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 |
| 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 | 8.13 | 9.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 9.14 |
| CHEMBL5177238 | — | — | 1 | 8.59 |
| CHEMBL5169992 | — | — | 1 | 8.49 |
| CHEMBL5197089 | — | — | 1 | 8.31 |
| CHEMBL5195670 | — | — | 1 | 8.24 |
| CHEMBL5206888 | — | — | 1 | 8.23 |
| CHEMBL5187230 | — | — | 1 | 8.22 |
| CHEMBL5195945 | — | — | 1 | 8.14 |
| CHEMBL5198054 | — | — | 1 | 7.75 |
| CHEMBL3301625 | SPEBRUTINIB | 2.0 | 1 | 7.66 |
| CHEMBL5201319 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL5177238 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5169992 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL5197089 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL5195670 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL5206888 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL5187230 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5195945 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL5198054 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3301625 | SPEBRUTINIB | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5201319 | — | IC50 | = | 219.0 | nM | 6.66 |