Assay Detail
Binding
CHEMBL4385484
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full-length human His-tagged BTK expressed in baculovirus expression system using FAM-Srctide peptide 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 | Binding |
| 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 | 8.68 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 10.00 |
| CHEMBL4520801 | — | — | 1 | 9.74 |
| CHEMBL4442732 | — | — | 1 | 9.60 |
| CHEMBL4436118 | — | — | 1 | 9.43 |
| CHEMBL4559065 | — | — | 1 | 9.39 |
| CHEMBL4456283 | — | — | 1 | 9.19 |
| CHEMBL4560385 | — | — | 1 | 8.82 |
| CHEMBL4440096 | — | — | 1 | 8.64 |
| CHEMBL4456974 | — | — | 1 | 8.59 |
| CHEMBL4556666 | — | — | 1 | 8.57 |
| CHEMBL4572913 | — | — | 1 | 8.43 |
| CHEMBL4591391 | — | — | 1 | 8.28 |
| CHEMBL4469663 | — | — | 1 | 8.21 |
| CHEMBL4462332 | — | — | 1 | 8.12 |
| CHEMBL4548556 | — | — | 1 | 7.21 |
| CHEMBL4518667 | — | — | 1 | 6.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4520801 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL4442732 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL4436118 | — | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL4559065 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL4456283 | — | IC50 | = | 0.64 | nM | 9.19 |
| CHEMBL4560385 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4440096 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4456974 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4556666 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4572913 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4591391 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4469663 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL4462332 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL4548556 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4518667 | — | IC50 | = | 247.0 | nM | 6.61 |