Assay Detail
Binding
CHEMBL3789511
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Inhibition of BTK (unknown origin)
15
Total Activities
15
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
Approaching the active conformation of 1,3-diaminopyrimidine based covalent inhibitors of Bruton's tyrosine kinase for treatment of Rheumatoid arthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.91 | 9.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3785165 | — | — | 1 | 9.04 |
| CHEMBL3787615 | — | — | 1 | 8.97 |
| CHEMBL3786931 | — | — | 1 | 8.83 |
| CHEMBL3786656 | — | — | 1 | 8.43 |
| CHEMBL3787191 | — | — | 1 | 8.39 |
| CHEMBL3301625 | SPEBRUTINIB | 2.0 | 1 | 8.34 |
| CHEMBL3787055 | — | — | 1 | 8.25 |
| CHEMBL3787531 | — | — | 1 | 8.18 |
| CHEMBL3785329 | — | — | 1 | 7.89 |
| CHEMBL3786922 | — | — | 1 | 7.51 |
| CHEMBL3787217 | — | — | 1 | 7.51 |
| CHEMBL3787671 | — | — | 1 | 7.51 |
| CHEMBL3787652 | — | — | 1 | 6.65 |
| CHEMBL3787293 | — | — | 1 | 6.58 |
| CHEMBL3785991 | — | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3785165 | — | IC50 | = | 0.903 | nM | 9.04 |
| CHEMBL3787615 | — | IC50 | = | 1.08 | nM | 8.97 |
| CHEMBL3786931 | — | IC50 | = | 1.48 | nM | 8.83 |
| CHEMBL3786656 | — | IC50 | = | 3.76 | nM | 8.43 |
| CHEMBL3787191 | — | IC50 | = | 4.11 | nM | 8.39 |
| CHEMBL3301625 | SPEBRUTINIB | IC50 | = | 4.61 | nM | 8.34 |
| CHEMBL3787055 | — | IC50 | = | 5.65 | nM | 8.25 |
| CHEMBL3787531 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL3785329 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3786922 | — | IC50 | = | 31.2 | nM | 7.51 |
| CHEMBL3787217 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3787671 | — | IC50 | = | 30.6 | nM | 7.51 |
| CHEMBL3787652 | — | IC50 | = | 222.0 | nM | 6.65 |
| CHEMBL3787293 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL3785991 | — | IC50 | = | 318.0 | nM | 6.50 |