Assay Detail
Binding
CHEMBL4201924
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal DYKDDDDK tagged biotinylated activated human recombinant BTK using FITC-labeled Srctide peptide substrate by mobility shift assay
33
Total Activities
33
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
Design and Synthesis of Novel Amino-triazine Analogues as Selective Bruton's Tyrosine Kinase Inhibitors for Treatment of Rheumatoid Arthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 7.14 | 9.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 9.27 |
| CHEMBL4211893 | — | — | 1 | 8.66 |
| CHEMBL4209441 | SOFNOBRUTINIB | 2.0 | 1 | 8.38 |
| CHEMBL4212436 | — | — | 1 | 8.29 |
| CHEMBL4208062 | — | — | 1 | 8.27 |
| CHEMBL4216339 | — | — | 1 | 8.20 |
| CHEMBL4204675 | — | — | 1 | 8.13 |
| CHEMBL4216862 | — | — | 1 | 8.08 |
| CHEMBL4203192 | — | — | 1 | 8.04 |
| CHEMBL4214343 | — | — | 1 | 8.03 |
| CHEMBL4217816 | — | — | 1 | 7.77 |
| CHEMBL4213416 | — | — | 1 | 7.55 |
| CHEMBL4209666 | — | — | 1 | 7.42 |
| CHEMBL4212860 | — | — | 1 | 7.38 |
| CHEMBL4218481 | — | — | 1 | 7.37 |
| CHEMBL4217003 | — | — | 1 | 7.37 |
| CHEMBL4217295 | — | — | 1 | 7.16 |
| CHEMBL4205287 | — | — | 1 | 7.09 |
| CHEMBL4205586 | — | — | 1 | 6.96 |
| CHEMBL4204802 | — | — | 1 | 6.85 |
| CHEMBL4209148 | — | — | 1 | 6.72 |
| CHEMBL4209020 | — | — | 1 | 6.55 |
| CHEMBL4204140 | — | — | 1 | 6.46 |
| CHEMBL4208482 | — | — | 1 | 6.19 |
| CHEMBL4215004 | — | — | 1 | 6.09 |
| CHEMBL4203409 | — | — | 1 | 5.75 |
| CHEMBL4215184 | — | — | 1 | 5.75 |
| CHEMBL4212668 | — | — | 1 | 5.60 |
| CHEMBL4210081 | — | — | 1 | 5.60 |
| CHEMBL4207762 | — | — | 1 | 5.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 0.54 | nM | 9.27 |
| CHEMBL4211893 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4209441 | SOFNOBRUTINIB | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4212436 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4208062 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4216339 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL4204675 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL4216862 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL4203192 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL4214343 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL4217816 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4213416 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4209666 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4212860 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4217003 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4218481 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4217295 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4205287 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4205586 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4204802 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4209148 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4209020 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4204140 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4208482 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL4215004 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4203409 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4215184 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4212668 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4210081 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4207762 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL4210252 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL4214068 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4213547 | — | IC50 | > | 10000.0 | nM | - |