Assay Detail
ADMET
CHEMBL4385485
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human EGFR cytoplasmic domain expressed in baculovirus expression system using FITC-C6-KKAEEEEYFELVAKK-NH2 as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by TR-FRET Lanthascreen assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.23 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4520801 | — | — | 1 | 7.82 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 7.75 |
| CHEMBL4442732 | — | — | 1 | 7.58 |
| CHEMBL4572913 | — | — | 1 | 6.83 |
| CHEMBL4559065 | — | — | 1 | 6.56 |
| CHEMBL4591391 | — | — | 1 | 6.24 |
| CHEMBL4436118 | — | — | 1 | 5.77 |
| CHEMBL4556666 | — | — | 1 | 5.66 |
| CHEMBL4440096 | — | — | 1 | 5.54 |
| CHEMBL4456283 | — | — | 1 | 5.41 |
| CHEMBL4469663 | — | — | 1 | 4.81 |
| CHEMBL4560385 | — | — | 1 | 4.78 |
| CHEMBL4462332 | — | — | 1 | - |
| CHEMBL4456974 | — | — | 1 | - |
| CHEMBL4518667 | — | — | 1 | - |
| CHEMBL4548556 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4520801 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4442732 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4572913 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL4559065 | — | IC50 | = | 274.0 | nM | 6.56 |
| CHEMBL4591391 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4436118 | — | IC50 | = | 1710.0 | nM | 5.77 |
| CHEMBL4556666 | — | IC50 | = | 2180.0 | nM | 5.66 |
| CHEMBL4440096 | — | IC50 | = | 2910.0 | nM | 5.54 |
| CHEMBL4456283 | — | IC50 | = | 3890.0 | nM | 5.41 |
| CHEMBL4469663 | — | IC50 | = | 15400.0 | nM | 4.81 |
| CHEMBL4560385 | — | IC50 | = | 16800.0 | nM | 4.78 |
| CHEMBL4462332 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4456974 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4518667 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4548556 | — | IC50 | > | 20000.0 | nM | - |