Assay Detail
Binding
CHEMBL4023698
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BTK in human whole blood-derived CD19+ B cells assessed as suppression of anti-IgM stimulated-CD69 expression preincubated for 1 hr followed by IgM stimulation for 18 hrs by FACS analysis
35
Total Activities
33
Compounds Tested
3
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 GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 7.41 | 8.34 |
| IC70 | 1 | - | - |
| IC90 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4085043 | — | — | 1 | 8.34 |
| CHEMBL4065122 | FENEBRUTINIB | 3.0 | 3 | 8.10 |
| CHEMBL4074792 | — | — | 1 | 7.99 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 7.92 |
| CHEMBL4092794 | — | — | 1 | 7.90 |
| CHEMBL4086408 | — | — | 1 | 7.81 |
| CHEMBL4087543 | — | — | 1 | 7.80 |
| CHEMBL4095248 | — | — | 1 | 7.79 |
| CHEMBL4095379 | — | — | 1 | 7.77 |
| CHEMBL4069790 | — | — | 1 | 7.63 |
| CHEMBL3670094 | — | — | 1 | 7.56 |
| CHEMBL4102992 | — | — | 1 | 7.56 |
| CHEMBL4090117 | — | — | 1 | 7.50 |
| CHEMBL4097832 | — | — | 1 | 7.49 |
| CHEMBL4071754 | — | — | 1 | 7.48 |
| CHEMBL3670095 | — | — | 1 | 7.44 |
| CHEMBL4062634 | — | — | 1 | 7.44 |
| CHEMBL4063638 | — | — | 1 | 7.41 |
| CHEMBL4066176 | — | — | 1 | 7.40 |
| CHEMBL4090946 | — | — | 1 | 7.37 |
| CHEMBL4070991 | — | — | 1 | 7.29 |
| CHEMBL4085477 | — | — | 1 | 7.26 |
| CHEMBL4093188 | — | — | 1 | 7.21 |
| CHEMBL4101904 | — | — | 1 | 7.19 |
| CHEMBL4060356 | — | — | 1 | 7.18 |
| CHEMBL4104307 | — | — | 1 | 7.11 |
| CHEMBL3952795 | — | — | 1 | 7.05 |
| CHEMBL4071161 | TIRABRUTINIB | 4.0 | 1 | 6.99 |
| CHEMBL4079803 | — | — | 1 | 6.93 |
| CHEMBL4075845 | — | — | 1 | 6.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4085043 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4065122 | FENEBRUTINIB | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4074792 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4092794 | — | IC50 | = | 12.7 | nM | 7.90 |
| CHEMBL4086408 | — | IC50 | = | 15.4 | nM | 7.81 |
| CHEMBL4087543 | — | IC50 | = | 15.9 | nM | 7.80 |
| CHEMBL4095248 | — | IC50 | = | 16.1 | nM | 7.79 |
| CHEMBL4095379 | — | IC50 | = | 16.9 | nM | 7.77 |
| CHEMBL4069790 | — | IC50 | = | 23.5 | nM | 7.63 |
| CHEMBL3670094 | — | IC50 | = | 27.6 | nM | 7.56 |
| CHEMBL4102992 | — | IC50 | = | 27.5 | nM | 7.56 |
| CHEMBL4090117 | — | IC50 | = | 31.6 | nM | 7.50 |
| CHEMBL4097832 | — | IC50 | = | 32.2 | nM | 7.49 |
| CHEMBL4071754 | — | IC50 | = | 33.4 | nM | 7.48 |
| CHEMBL3670095 | — | IC50 | = | 36.5 | nM | 7.44 |
| CHEMBL4062634 | — | IC50 | = | 36.6 | nM | 7.44 |
| CHEMBL4063638 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4066176 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4090946 | — | IC50 | = | 42.4 | nM | 7.37 |
| CHEMBL4070991 | — | IC50 | = | 51.5 | nM | 7.29 |
| CHEMBL4085477 | — | IC50 | = | 54.9 | nM | 7.26 |
| CHEMBL4093188 | — | IC50 | = | 61.9 | nM | 7.21 |
| CHEMBL4101904 | — | IC50 | = | 64.4 | nM | 7.19 |
| CHEMBL4060356 | — | IC50 | = | 66.5 | nM | 7.18 |
| CHEMBL4104307 | — | IC50 | = | 77.8 | nM | 7.11 |
| CHEMBL3952795 | — | IC50 | = | 88.3 | nM | 7.05 |
| CHEMBL4071161 | TIRABRUTINIB | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL4079803 | — | IC50 | = | 116.1 | nM | 6.93 |
| CHEMBL4075845 | — | IC50 | = | 121.1 | nM | 6.92 |
| CHEMBL3707348 | ACALABRUTINIB | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL4082268 | — | IC50 | = | 240.9 | nM | 6.62 |
| CHEMBL4075253 | — | IC50 | = | 387.0 | nM | 6.41 |
| CHEMBL4065122 | FENEBRUTINIB | IC70 | = | 27.0 | nM | - |
| CHEMBL4065122 | FENEBRUTINIB | IC90 | = | 135.0 | nM | - |