Assay Detail
Binding
CHEMBL4130922
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant full length His-tagged human BLK expressed in baculovirus expression system using poly (4:1 Glu, Tyr) as substrate preincubated for 1 hr followed by substrate addition measured after 1 hr by ADP-glo assay
23
Total Activities
23
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
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 |
|---|---|---|---|
| IC50 | 23 | 6.46 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4075449 | — | — | 1 | 7.52 |
| CHEMBL4068097 | — | — | 1 | 7.08 |
| CHEMBL4163217 | — | — | 1 | 6.80 |
| CHEMBL4077107 | — | — | 1 | 6.75 |
| CHEMBL4171756 | — | — | 1 | 6.72 |
| CHEMBL4160923 | — | — | 1 | 6.61 |
| CHEMBL4162994 | — | — | 1 | 6.60 |
| CHEMBL4161110 | — | — | 1 | 6.53 |
| CHEMBL4071759 | — | — | 1 | 6.53 |
| CHEMBL4161149 | — | — | 1 | 6.52 |
| CHEMBL4173695 | — | — | 1 | 6.47 |
| CHEMBL4166849 | — | — | 1 | 6.47 |
| CHEMBL4098453 | — | — | 1 | 6.47 |
| CHEMBL4077064 | — | — | 1 | 6.44 |
| CHEMBL4091991 | — | — | 1 | 6.42 |
| CHEMBL4170077 | — | — | 1 | 6.22 |
| CHEMBL4159459 | — | — | 1 | 5.95 |
| CHEMBL4163399 | — | — | 1 | 5.71 |
| CHEMBL4159852 | — | — | 1 | 5.69 |
| CHEMBL4159628 | — | — | 1 | 5.68 |
| CHEMBL4166664 | — | — | 1 | - |
| CHEMBL4174577 | — | — | 1 | - |
| CHEMBL4175202 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4075449 | — | IC50 | = | 30.2 | nM | 7.52 |
| CHEMBL4068097 | — | IC50 | = | 83.6 | nM | 7.08 |
| CHEMBL4163217 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4077107 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL4171756 | — | IC50 | = | 191.0 | nM | 6.72 |
| CHEMBL4160923 | — | IC50 | = | 246.0 | nM | 6.61 |
| CHEMBL4162994 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4161110 | — | IC50 | = | 293.0 | nM | 6.53 |
| CHEMBL4071759 | — | IC50 | = | 295.0 | nM | 6.53 |
| CHEMBL4161149 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4173695 | — | IC50 | = | 342.0 | nM | 6.47 |
| CHEMBL4166849 | — | IC50 | = | 336.0 | nM | 6.47 |
| CHEMBL4098453 | — | IC50 | = | 339.0 | nM | 6.47 |
| CHEMBL4077064 | — | IC50 | = | 366.0 | nM | 6.44 |
| CHEMBL4091991 | — | IC50 | = | 377.0 | nM | 6.42 |
| CHEMBL4170077 | — | IC50 | = | 607.0 | nM | 6.22 |
| CHEMBL4159459 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL4163399 | — | IC50 | = | 1950.0 | nM | 5.71 |
| CHEMBL4159852 | — | IC50 | = | 2060.0 | nM | 5.69 |
| CHEMBL4159628 | — | IC50 | = | 2090.0 | nM | 5.68 |
| CHEMBL4166664 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4174577 | — | IC50 | - | — | - | |
| CHEMBL4175202 | — | IC50 | > | 10000.0 | nM | - |