Assay Detail
Binding
CHEMBL4264020
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length human BTK (8 to 80 residues) using FITC-AHA-EEPLYWSFPAKKK-NH2 as substrate after 90 mins by off-chip mobility shift assay
9
Total Activities
9
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
Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.71 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4288997 | — | — | 1 | 9.10 |
| CHEMBL4278321 | — | — | 1 | 8.89 |
| CHEMBL4281335 | — | — | 1 | 8.89 |
| CHEMBL4245727 | — | — | 1 | 8.80 |
| CHEMBL4282893 | — | — | 1 | 8.72 |
| CHEMBL4286628 | — | — | 1 | 8.66 |
| CHEMBL4278717 | — | — | 1 | 8.64 |
| CHEMBL4285083 | — | — | 1 | 8.55 |
| CHEMBL4290066 | — | — | 1 | 8.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4288997 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4278321 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4281335 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4245727 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4282893 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4286628 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4278717 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4285083 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4290066 | — | IC50 | = | 7.5 | nM | 8.12 |