Assay Detail
Binding
CHEMBL4023697
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant C-terminal polyhistidine tagged BTK (1 to 659 residues)-mediated synthetic peptide substrate phosphorylation expressed in baculovirus-infected insect cells
28
Total Activities
28
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
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 |
|---|---|---|---|
| Ki | 28 | 8.90 | 9.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4102992 | — | — | 1 | 9.49 |
| CHEMBL3670094 | — | — | 1 | 9.46 |
| CHEMBL4095379 | — | — | 1 | 9.43 |
| CHEMBL4092794 | — | — | 1 | 9.37 |
| CHEMBL4069790 | — | — | 1 | 9.37 |
| CHEMBL4090117 | — | — | 1 | 9.35 |
| CHEMBL4063638 | — | — | 1 | 9.24 |
| CHEMBL4085043 | — | — | 1 | 9.19 |
| CHEMBL3670095 | — | — | 1 | 9.16 |
| CHEMBL4070991 | — | — | 1 | 9.10 |
| CHEMBL4065122 | FENEBRUTINIB | 3.0 | 1 | 9.04 |
| CHEMBL4087543 | — | — | 1 | 9.02 |
| CHEMBL4097832 | — | — | 1 | 9.00 |
| CHEMBL4093188 | — | — | 1 | 9.00 |
| CHEMBL4062634 | — | — | 1 | 8.92 |
| CHEMBL4074792 | — | — | 1 | 8.89 |
| CHEMBL4060356 | — | — | 1 | 8.74 |
| CHEMBL4082268 | — | — | 1 | 8.74 |
| CHEMBL4086408 | — | — | 1 | 8.74 |
| CHEMBL4066176 | — | — | 1 | 8.74 |
| CHEMBL4085477 | — | — | 1 | 8.74 |
| CHEMBL4090946 | — | — | 1 | 8.60 |
| CHEMBL4071754 | — | — | 1 | 8.48 |
| CHEMBL4079803 | — | — | 1 | 8.40 |
| CHEMBL4104307 | — | — | 1 | 8.38 |
| CHEMBL4075845 | — | — | 1 | 8.22 |
| CHEMBL4101904 | — | — | 1 | 8.20 |
| CHEMBL4075253 | — | — | 1 | 8.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4102992 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL3670094 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL4095379 | — | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL4092794 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL4069790 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL4090117 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL4063638 | — | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL4085043 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL3670095 | — | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL4070991 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL4065122 | FENEBRUTINIB | Ki | = | 0.91 | nM | 9.04 |
| CHEMBL4087543 | — | Ki | = | 0.96 | nM | 9.02 |
| CHEMBL4097832 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4093188 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4062634 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL4074792 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL4060356 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL4082268 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL4086408 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL4066176 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL4085477 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL4090946 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL4071754 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL4079803 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4104307 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL4075845 | — | Ki | = | 5.97 | nM | 8.22 |
| CHEMBL4101904 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL4075253 | — | Ki | = | 6.9 | nM | 8.16 |