Assay Detail
Binding
CHEMBL4201925
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal DYKDDDDK tagged biotinylated unactivated human recombinant BTK using FITC-labeled Srctide peptide substrate by 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 | 8.59 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 9.48 |
| CHEMBL4204675 | — | — | 1 | 9.41 |
| CHEMBL4209441 | SOFNOBRUTINIB | 2.0 | 1 | 9.41 |
| CHEMBL4217816 | — | — | 1 | 9.39 |
| CHEMBL4211893 | — | — | 1 | 9.31 |
| CHEMBL4214343 | — | — | 1 | 9.29 |
| CHEMBL4208062 | — | — | 1 | 9.28 |
| CHEMBL4212436 | — | — | 1 | 9.27 |
| CHEMBL4216339 | — | — | 1 | 9.24 |
| CHEMBL4216862 | — | — | 1 | 9.24 |
| CHEMBL4212860 | — | — | 1 | 9.21 |
| CHEMBL4209148 | — | — | 1 | 9.17 |
| CHEMBL4217003 | — | — | 1 | 9.13 |
| CHEMBL4213416 | — | — | 1 | 9.09 |
| CHEMBL4203192 | — | — | 1 | 9.07 |
| CHEMBL4205586 | — | — | 1 | 8.80 |
| CHEMBL4204802 | — | — | 1 | 8.68 |
| CHEMBL4217295 | — | — | 1 | 8.66 |
| CHEMBL4203409 | — | — | 1 | 8.64 |
| CHEMBL4205287 | — | — | 1 | 8.60 |
| CHEMBL4208482 | — | — | 1 | 8.42 |
| CHEMBL4215004 | — | — | 1 | 8.40 |
| CHEMBL4204140 | — | — | 1 | 8.38 |
| CHEMBL4209020 | — | — | 1 | 8.37 |
| CHEMBL4209666 | — | — | 1 | 8.33 |
| CHEMBL4215184 | — | — | 1 | 8.19 |
| CHEMBL4207762 | — | — | 1 | 8.00 |
| CHEMBL4210081 | — | — | 1 | 7.82 |
| CHEMBL4210252 | — | — | 1 | 7.47 |
| CHEMBL4214068 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL4204675 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL4209441 | SOFNOBRUTINIB | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL4217816 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL4211893 | — | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL4214343 | — | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL4208062 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL4212436 | — | IC50 | = | 0.54 | nM | 9.27 |
| CHEMBL4216339 | — | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL4216862 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL4212860 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL4209148 | — | IC50 | = | 0.67 | nM | 9.17 |
| CHEMBL4217003 | — | IC50 | = | 0.74 | nM | 9.13 |
| CHEMBL4213416 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL4203192 | — | IC50 | = | 0.86 | nM | 9.07 |
| CHEMBL4205586 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4204802 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4217295 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4203409 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4205287 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4208482 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4215004 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4204140 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4209020 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4209666 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL4215184 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4207762 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4210081 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4210252 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4214068 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4212668 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4213547 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL4218481 | — | IC50 | < | 0.3 | nM | - |