Assay Detail
Binding
CHEMBL4672804
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Inhibition of BTK in human Ramos B cells assessed as reduction in goat anti human IgM-stimulated calcium flux preincubated for 1 hr followed by goat anti human IgM addition and measured for 180 secs by FLIPR assay
20
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Ramos |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTK.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.72 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4741099 | — | — | 1 | 8.51 |
| CHEMBL3891545 | — | — | 4 | 8.18 |
| CHEMBL3928976 | — | — | 4 | 8.16 |
| CHEMBL4741884 | — | — | 2 | 8.07 |
| CHEMBL4751952 | — | — | 3 | 7.92 |
| CHEMBL4743497 | — | — | 3 | 7.85 |
| CHEMBL4789404 | — | — | 1 | 7.72 |
| CHEMBL4754459 | — | — | 1 | 7.72 |
| CHEMBL3918580 | — | — | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4741099 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3891545 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL3928976 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL3891545 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL4741884 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3928976 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4751952 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4751952 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4743497 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4751952 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4743497 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4743497 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4754459 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4789404 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4741884 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3918580 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3928976 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL3891545 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3891545 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3928976 | — | IC50 | > | 300.0 | nM | - |