Assay Detail
Binding
CHEMBL4057947
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant full-length His6-tagged BTK (unknown origin) expressed in baculovirus infected Sf9 cells using biotinylated A5 peptide as substrate preincubated for 60 mins followed by substrate addition measured after 120 mins by LANCE TR-FRET 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
Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 8.73 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4079820 | — | — | 1 | 10.00 |
| CHEMBL4076024 | — | — | 1 | 9.70 |
| CHEMBL4069387 | — | — | 1 | 9.60 |
| CHEMBL4094125 | — | — | 1 | 9.52 |
| CHEMBL4081661 | — | — | 1 | 9.52 |
| CHEMBL4062498 | — | — | 1 | 9.43 |
| CHEMBL4096669 | — | — | 1 | 9.40 |
| CHEMBL4075954 | — | — | 1 | 9.40 |
| CHEMBL4065907 | — | — | 1 | 9.40 |
| CHEMBL4060757 | — | — | 1 | 9.23 |
| CHEMBL4059723 | — | — | 1 | 9.15 |
| CHEMBL4077588 | — | — | 1 | 9.10 |
| CHEMBL4075605 | — | — | 1 | 9.05 |
| CHEMBL4104254 | — | — | 1 | 8.92 |
| CHEMBL4097247 | — | — | 1 | 8.48 |
| CHEMBL4078497 | — | — | 1 | 8.47 |
| CHEMBL4099975 | — | — | 1 | 8.28 |
| CHEMBL4086348 | — | — | 1 | 8.23 |
| CHEMBL4079225 | — | — | 1 | 8.18 |
| CHEMBL4096526 | — | — | 1 | 7.97 |
| CHEMBL4066585 | — | — | 1 | 6.88 |
| CHEMBL4104951 | — | — | 1 | 6.53 |
| CHEMBL4087095 | — | — | 1 | 6.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4079820 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4076024 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4069387 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL4094125 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4081661 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4062498 | — | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL4096669 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4075954 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4065907 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4060757 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL4059723 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4077588 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4075605 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4104254 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4097247 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4078497 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4099975 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4086348 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL4079225 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL4096526 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL4066585 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL4104951 | — | IC50 | = | 294.0 | nM | 6.53 |
| CHEMBL4087095 | — | IC50 | = | 377.0 | nM | 6.42 |