Assay Detail
Binding
CHEMBL4130923
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant GST-tagged human JAK3 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 | 6.38 | 7.76 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4159628 | — | — | 1 | 7.76 |
| CHEMBL4162994 | — | — | 1 | 7.60 |
| CHEMBL4075449 | — | — | 1 | 7.42 |
| CHEMBL4173695 | — | — | 1 | 7.41 |
| CHEMBL4091991 | — | — | 1 | 6.76 |
| CHEMBL4077107 | — | — | 1 | 6.75 |
| CHEMBL4163217 | — | — | 1 | 6.72 |
| CHEMBL4159459 | — | — | 1 | 6.66 |
| CHEMBL4161110 | — | — | 1 | 6.65 |
| CHEMBL4098453 | — | — | 1 | 6.46 |
| CHEMBL4159852 | — | — | 1 | 6.19 |
| CHEMBL4166849 | — | — | 1 | 6.18 |
| CHEMBL4171756 | — | — | 1 | 6.01 |
| CHEMBL4071759 | — | — | 1 | 6.01 |
| CHEMBL4163399 | — | — | 1 | 5.82 |
| CHEMBL4175202 | — | — | 1 | 5.81 |
| CHEMBL4160923 | — | — | 1 | 5.67 |
| CHEMBL4077064 | — | — | 1 | 5.29 |
| CHEMBL4170077 | — | — | 1 | 5.25 |
| CHEMBL4161149 | — | — | 1 | 5.25 |
| CHEMBL4174577 | — | — | 1 | - |
| CHEMBL4068097 | — | — | 1 | - |
| CHEMBL4166664 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4159628 | — | IC50 | = | 17.4 | nM | 7.76 |
| CHEMBL4162994 | — | IC50 | = | 25.3 | nM | 7.60 |
| CHEMBL4075449 | — | IC50 | = | 38.1 | nM | 7.42 |
| CHEMBL4173695 | — | IC50 | = | 38.6 | nM | 7.41 |
| CHEMBL4091991 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL4077107 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL4163217 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL4159459 | — | IC50 | = | 218.0 | nM | 6.66 |
| CHEMBL4161110 | — | IC50 | = | 224.0 | nM | 6.65 |
| CHEMBL4098453 | — | IC50 | = | 343.0 | nM | 6.46 |
| CHEMBL4159852 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL4166849 | — | IC50 | = | 654.0 | nM | 6.18 |
| CHEMBL4171756 | — | IC50 | = | 983.0 | nM | 6.01 |
| CHEMBL4071759 | — | IC50 | = | 983.0 | nM | 6.01 |
| CHEMBL4163399 | — | IC50 | = | 1520.0 | nM | 5.82 |
| CHEMBL4175202 | — | IC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL4160923 | — | IC50 | = | 2150.0 | nM | 5.67 |
| CHEMBL4077064 | — | IC50 | = | 5180.0 | nM | 5.29 |
| CHEMBL4170077 | — | IC50 | = | 5580.0 | nM | 5.25 |
| CHEMBL4161149 | — | IC50 | = | 5640.0 | nM | 5.25 |
| CHEMBL4174577 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4068097 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4166664 | — | IC50 | > | 10000.0 | nM | - |