Assay Detail
Binding
CHEMBL4264696
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human full length N-terminal GST-tagged BTK (2 to 659 residues) expressed in baculovirus expression system using FITC-AHA-EEPLYWSFPAKKK-NH2 substrate measured after 90 mins by off-chip mobility shift assay
20
Total Activities
20
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
Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 8.47 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4279353 | — | — | 1 | 10.05 |
| CHEMBL4276669 | — | — | 1 | 10.00 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 9.70 |
| CHEMBL4279430 | — | — | 1 | 9.52 |
| CHEMBL4290540 | — | — | 1 | 9.30 |
| CHEMBL4281335 | — | — | 1 | 9.22 |
| CHEMBL4277754 | — | — | 1 | 8.96 |
| CHEMBL4292583 | — | — | 1 | 8.89 |
| CHEMBL4245727 | — | — | 1 | 8.82 |
| CHEMBL4285813 | — | — | 1 | 8.80 |
| CHEMBL4277875 | — | — | 1 | 8.72 |
| CHEMBL4291033 | — | — | 1 | 8.10 |
| CHEMBL4280401 | — | — | 1 | 7.96 |
| CHEMBL4286664 | — | — | 1 | 7.80 |
| CHEMBL4293010 | — | — | 1 | 7.79 |
| CHEMBL4287216 | — | — | 1 | 6.75 |
| CHEMBL4282745 | — | — | 1 | 6.30 |
| CHEMBL4289625 | — | — | 1 | 5.80 |
| CHEMBL4279288 | — | — | 1 | - |
| CHEMBL4290625 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4279353 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL4276669 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4279430 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4290540 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4281335 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4277754 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4292583 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4245727 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4285813 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4277875 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4291033 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4280401 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4286664 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4293010 | — | IC50 | = | 16.2 | nM | 7.79 |
| CHEMBL4287216 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4282745 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4289625 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4279288 | — | IC50 | > | 6000.0 | nM | - |
| CHEMBL4290625 | — | IC50 | > | 6000.0 | nM | - |