Assay Detail
Binding
CHEMBL4668253
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length human unphosphorylated BTK using FITC-Ahx-TSELKKVVALYDYMPMNAND-NH2 as substrate incubated for 60 mins in presence of ATP at Km concentration
14
Total Activities
14
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
Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 8.19 | 10.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4762397 | — | — | 1 | 10.85 |
| CHEMBL4749522 | — | — | 1 | 9.22 |
| CHEMBL4593663 | — | — | 1 | 9.05 |
| CHEMBL4739958 | — | — | 1 | 9.00 |
| CHEMBL4795673 | — | — | 1 | 8.92 |
| CHEMBL4746262 | — | — | 1 | 8.85 |
| CHEMBL4740933 | — | — | 1 | 8.30 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 8.30 |
| CHEMBL4789435 | — | — | 1 | 8.22 |
| CHEMBL4566818 | — | — | 1 | 7.89 |
| CHEMBL4793026 | — | — | 1 | 7.58 |
| CHEMBL4788086 | — | — | 1 | 6.72 |
| CHEMBL4744271 | — | — | 1 | 6.41 |
| CHEMBL4752522 | — | — | 1 | 5.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4762397 | — | IC50 | = | 0.014 | nM | 10.85 |
| CHEMBL4749522 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4593663 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4739958 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4795673 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4746262 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4740933 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4789435 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4566818 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4793026 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4788086 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4744271 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4752522 | — | IC50 | = | 3900.0 | nM | 5.41 |