Assay Detail
Binding
CHEMBL4622573
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Inhibition of BTK in human whole blood assessed as reduction in autophosphorylation at Y223 residue incubated for 1 hr by mesoscale assay
28
Total Activities
28
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
Stereochemical Differences in Fluorocyclopropyl Amides Enable Tuning of Btk Inhibition and Off-Target Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.71 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4638277 | — | — | 1 | 8.72 |
| CHEMBL4643319 | — | — | 1 | 8.70 |
| CHEMBL4065122 | FENEBRUTINIB | 3.0 | 1 | 8.64 |
| CHEMBL4644207 | — | — | 1 | 8.64 |
| CHEMBL4634904 | — | — | 1 | 8.62 |
| CHEMBL4648439 | — | — | 1 | 8.49 |
| CHEMBL4644448 | — | — | 1 | 8.42 |
| CHEMBL4641507 | — | — | 1 | 8.32 |
| CHEMBL4646964 | — | — | 1 | 8.29 |
| CHEMBL4644856 | — | — | 1 | 8.15 |
| CHEMBL4638307 | — | — | 1 | 8.14 |
| CHEMBL4649410 | — | — | 1 | 8.11 |
| CHEMBL4638562 | — | — | 1 | 7.92 |
| CHEMBL4648782 | — | — | 1 | 7.85 |
| CHEMBL4646782 | — | — | 1 | 7.82 |
| CHEMBL4647342 | — | — | 1 | 7.66 |
| CHEMBL4647569 | — | — | 1 | 7.58 |
| CHEMBL4633058 | — | — | 1 | 7.50 |
| CHEMBL4649614 | — | — | 1 | 7.36 |
| CHEMBL4636316 | — | — | 1 | 7.22 |
| CHEMBL4640083 | — | — | 1 | 7.13 |
| CHEMBL4638921 | — | — | 1 | 7.13 |
| CHEMBL4638609 | — | — | 1 | 7.01 |
| CHEMBL4639728 | — | — | 1 | 6.70 |
| CHEMBL4643339 | — | — | 1 | 6.55 |
| CHEMBL4646580 | — | — | 1 | 6.50 |
| CHEMBL4638802 | — | — | 1 | 6.44 |
| CHEMBL4643297 | — | — | 1 | 6.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4638277 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4643319 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4065122 | FENEBRUTINIB | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4644207 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4634904 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4648439 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4644448 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4641507 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4646964 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4644856 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL4638307 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4649410 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL4638562 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4648782 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4646782 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4647342 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4647569 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4633058 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4649614 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4636316 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4640083 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4638921 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4638609 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4639728 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4643339 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4646580 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4638802 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4643297 | — | IC50 | = | 410.0 | nM | 6.39 |