Assay Detail
Binding
CHEMBL4818907
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Covalent inhibition of recombinant human GST-tagged BTK (2 to 659 end residues) expressed in baculovirus expression system assessed as inhibition constant using NH2-KKKAPFSWYLPEEG as substrate measured every 2 mins for 2 hrs in presence of ATP by microplate reader assay
16
Total Activities
15
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 Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase with Oral Anti-Inflammatory Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 6.83 | 8.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4853403 | — | — | 2 | 8.32 |
| CHEMBL4854911 | — | — | 1 | 8.04 |
| CHEMBL4846828 | — | — | 1 | 7.93 |
| CHEMBL4875401 | — | — | 1 | 7.91 |
| CHEMBL4849068 | — | — | 1 | 7.83 |
| CHEMBL4851021 | — | — | 1 | 7.54 |
| CHEMBL4852459 | — | — | 1 | 7.29 |
| CHEMBL4861899 | — | — | 1 | 6.85 |
| CHEMBL4871745 | — | — | 1 | 6.66 |
| CHEMBL4871385 | — | — | 1 | 6.47 |
| CHEMBL4877611 | — | — | 1 | 5.80 |
| CHEMBL4863521 | — | — | 1 | 5.73 |
| CHEMBL4877368 | — | — | 1 | 5.48 |
| CHEMBL4853953 | — | — | 1 | 5.38 |
| CHEMBL4873622 | — | — | 1 | 5.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4853403 | — | Ki | = | 4.81 | nM | 8.32 |
| CHEMBL4854911 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL4846828 | — | Ki | = | 11.7 | nM | 7.93 |
| CHEMBL4875401 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL4849068 | — | Ki | = | 14.8 | nM | 7.83 |
| CHEMBL4851021 | — | Ki | = | 28.8 | nM | 7.54 |
| CHEMBL4852459 | — | Ki | = | 51.9 | nM | 7.29 |
| CHEMBL4861899 | — | Ki | = | 141.0 | nM | 6.85 |
| CHEMBL4853403 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL4871745 | — | Ki | = | 217.0 | nM | 6.66 |
| CHEMBL4871385 | — | Ki | = | 337.0 | nM | 6.47 |
| CHEMBL4877611 | — | Ki | = | 1580.0 | nM | 5.80 |
| CHEMBL4863521 | — | Ki | = | 1850.0 | nM | 5.73 |
| CHEMBL4877368 | — | Ki | = | 3290.0 | nM | 5.48 |
| CHEMBL4853953 | — | Ki | = | 4220.0 | nM | 5.38 |
| CHEMBL4873622 | — | Ki | = | 6420.0 | nM | 5.19 |