Assay Detail
Binding
CHEMBL5579110
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Covalent inhibition of full-length BTK (unknown origin) expressed in Escherichia coli BL21 (DE3) incubated for 1 hr in presence of ATP by ADP-Glo kinase assay
5
Total Activities
5
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 | 5 | 7.58 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 8.05 |
| CHEMBL5593141 | — | — | 1 | 7.62 |
| CHEMBL5589636 | — | — | 1 | 7.55 |
| CHEMBL5589957 | — | — | 1 | 7.46 |
| CHEMBL5590893 | — | — | 1 | 7.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5593141 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5589636 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5589957 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5590893 | — | IC50 | = | 57.0 | nM | 7.24 |