Assay Detail
Binding
CHEMBL5579115
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Covalent inhibition of full length N-terminal GST tagged BTK (2 to 659 residues) (unknown origin) using AQT0101 as substrate preincubated for 60 mins in presence of ATP by microplate reader analysis
4
Total Activities
4
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
Exploring 2-Sulfonylpyrimidine Warheads as Acrylamide Surrogates for Targeted Covalent Inhibition: A BTK Story.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 9.16 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 10.00 |
| CHEMBL5593141 | — | — | 1 | 9.51 |
| CHEMBL5589636 | — | — | 1 | 8.92 |
| CHEMBL5590893 | — | — | 1 | 8.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5593141 | — | IC50 | = | 0.31 | nM | 9.51 |
| CHEMBL5589636 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5590893 | — | IC50 | = | 6.3 | nM | 8.20 |