Assay Detail
Binding
CHEMBL4429374
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Inhibition of BTK in human RamosB cells assessed as suppression of BCR/anti-IgM stimulated calcium flux pre-incubated for 1 hr followed by BCR/anti-IgM stimulation
13
Total Activities
13
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
Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.27 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4473176 | — | — | 1 | 7.75 |
| CHEMBL4550390 | — | — | 1 | 7.66 |
| CHEMBL4467132 | — | — | 1 | 7.62 |
| CHEMBL4465380 | — | — | 1 | 7.58 |
| CHEMBL3918580 | — | — | 1 | 7.58 |
| CHEMBL3977725 | — | — | 1 | 7.52 |
| CHEMBL4460221 | — | — | 1 | 7.47 |
| CHEMBL4513599 | — | — | 1 | 7.40 |
| CHEMBL4543505 | — | — | 1 | 7.32 |
| CHEMBL4554269 | — | — | 1 | 6.84 |
| CHEMBL4439761 | — | — | 1 | 6.81 |
| CHEMBL4567605 | — | — | 1 | 6.62 |
| CHEMBL3939772 | — | — | 1 | 6.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4473176 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4550390 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4467132 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4465380 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3918580 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3977725 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4460221 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4513599 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4543505 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4554269 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL4439761 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL4567605 | — | IC50 | = | 238.0 | nM | 6.62 |
| CHEMBL3939772 | — | IC50 | = | 410.0 | nM | 6.39 |