Assay Detail
Binding
CHEMBL4375192
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Covalent inhibition of N-terminal GST-fused human BTK (2-659(end) amino acids) expressed in baculovirus expression system using FITC-AHA-EEPLYWSFPAKKK-NH2 as substrate incubated for 90 mins by microfluidic off-Chip Mobility Shift Assay
31
Total Activities
31
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 Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 7.75 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4543998 | — | — | 1 | 9.70 |
| CHEMBL4466205 | — | — | 1 | 9.70 |
| CHEMBL4532368 | — | — | 1 | 9.22 |
| CHEMBL4459438 | — | — | 1 | 9.10 |
| CHEMBL4515024 | — | — | 1 | 8.68 |
| CHEMBL4528630 | — | — | 1 | 8.54 |
| CHEMBL4554990 | — | — | 1 | 8.40 |
| CHEMBL4461455 | — | — | 1 | 8.30 |
| CHEMBL4469004 | — | — | 1 | 8.26 |
| CHEMBL4476695 | — | — | 1 | 8.23 |
| CHEMBL4468148 | — | — | 1 | 8.19 |
| CHEMBL4436563 | — | — | 1 | 8.10 |
| CHEMBL4072833 | EVOBRUTINIB | 3.0 | 1 | 8.05 |
| CHEMBL4548457 | — | — | 1 | 8.05 |
| CHEMBL4441219 | — | — | 1 | 8.00 |
| CHEMBL4469908 | — | — | 1 | 7.85 |
| CHEMBL4537274 | — | — | 1 | 7.75 |
| CHEMBL4542934 | — | — | 1 | 7.68 |
| CHEMBL4550271 | — | — | 1 | 7.64 |
| CHEMBL4475457 | — | — | 1 | 7.48 |
| CHEMBL4588680 | — | — | 1 | 7.36 |
| CHEMBL4539748 | — | — | 1 | 6.82 |
| CHEMBL4453568 | — | — | 1 | 6.80 |
| CHEMBL4587672 | — | — | 1 | 6.54 |
| CHEMBL47940 | — | — | 1 | 6.51 |
| CHEMBL4572535 | — | — | 1 | 6.14 |
| CHEMBL4472627 | — | — | 1 | 5.92 |
| CHEMBL4586433 | — | — | 1 | 5.82 |
| CHEMBL4558157 | — | — | 1 | 5.82 |
| CHEMBL4553343 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4543998 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4466205 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4532368 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4459438 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4515024 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4528630 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4554990 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4461455 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4469004 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL4476695 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL4468148 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4436563 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4072833 | EVOBRUTINIB | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL4548457 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4441219 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL4469908 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4537274 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4542934 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4550271 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4475457 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4588680 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4539748 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4453568 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4587672 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL47940 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4572535 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL4472627 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4586433 | — | IC50 | = | 1510.0 | nM | 5.82 |
| CHEMBL4558157 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4553343 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4547696 | — | IC50 | > | 100000.0 | nM | - |