Assay Detail
Binding
CHEMBL4672805
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BTK in human whole blood assessed as reduction in goat anti human IgM/human IL4-stimulated CD69 cell surface expression on peripheral B cells incubated for 18 hrs by FACS analysis
20
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| 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 | 6.89 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3928976 | — | — | 4 | 7.60 |
| CHEMBL3891545 | — | — | 4 | 7.43 |
| CHEMBL4751952 | — | — | 3 | 7.16 |
| CHEMBL4743497 | — | — | 3 | 7.12 |
| CHEMBL4789404 | — | — | 1 | 6.85 |
| CHEMBL4754459 | — | — | 1 | 6.85 |
| CHEMBL4741884 | — | — | 2 | 6.39 |
| CHEMBL3918580 | — | — | 1 | 6.26 |
| CHEMBL4741099 | — | — | 1 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3928976 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3891545 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3891545 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4751952 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4743497 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4751952 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4743497 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4743497 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4751952 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4789404 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4754459 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3928976 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL4741884 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL3918580 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4741099 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3928976 | — | IC50 | - | — | - | |
| CHEMBL3928976 | — | IC50 | - | — | - | |
| CHEMBL3891545 | — | IC50 | - | — | - | |
| CHEMBL3891545 | — | IC50 | - | — | - | |
| CHEMBL4741884 | — | IC50 | - | — | - |