Assay Detail
Binding
CHEMBL4130925
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Irreversible inhibition of recombinant full length His-tagged human BTK expressed in baculovirus expression system using poly (4:1 Glu, Tyr) as substrate preincubated for 2 to 60 mins followed by substrate addition measured after 1 hr by ADP-glo assay
8
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton's tyrosine kinase (BTK) irreversible inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 8.01 | 8.70 |
| Kinact | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4075449 | — | — | 2 | 8.70 |
| CHEMBL4091991 | — | — | 2 | 8.49 |
| CHEMBL4077064 | — | — | 2 | 7.85 |
| CHEMBL4166664 | — | — | 2 | 7.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4075449 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4091991 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL4077064 | — | Ki | = | 14.2 | nM | 7.85 |
| CHEMBL4166664 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL4075449 | — | Kinact | = | 0.14 | /min | - |
| CHEMBL4166664 | — | Kinact | = | 0.07 | /min | - |
| CHEMBL4091991 | — | Kinact | = | 0.15 | /min | - |
| CHEMBL4077064 | — | Kinact | = | 0.13 | /min | - |