Assay Detail
Binding
CHEMBL3407032
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Inhibition of BTK (unknown origin) after 1 hr by TR-FRET analysis
32
Total Activities
32
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 novel Bruton's tyrosine kinase (BTK) inhibitors bearing a pyrrolo[2,3-d]pyrimidine scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 7.30 | 8.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3402585 | — | — | 1 | 8.32 |
| CHEMBL3402584 | — | — | 1 | 8.15 |
| CHEMBL2057918 | — | — | 1 | 7.88 |
| CHEMBL3402583 | — | — | 1 | 7.82 |
| CHEMBL3400174 | — | — | 1 | 7.80 |
| CHEMBL3402587 | — | — | 1 | 7.78 |
| CHEMBL3400979 | — | — | 1 | 7.75 |
| CHEMBL3402569 | — | — | 1 | 7.74 |
| CHEMBL3402576 | — | — | 1 | 7.67 |
| CHEMBL3402588 | — | — | 1 | 7.61 |
| CHEMBL3402586 | — | — | 1 | 7.60 |
| CHEMBL3402571 | — | — | 1 | 7.50 |
| CHEMBL3402581 | — | — | 1 | 7.49 |
| CHEMBL3402575 | — | — | 1 | 7.41 |
| CHEMBL3400978 | — | — | 1 | 7.38 |
| CHEMBL3402589 | — | — | 1 | 7.34 |
| CHEMBL3402570 | — | — | 1 | 7.29 |
| CHEMBL3402582 | — | — | 1 | 7.24 |
| CHEMBL3400976 | — | — | 1 | 7.23 |
| CHEMBL3402572 | — | — | 1 | 7.20 |
| CHEMBL3402580 | — | — | 1 | 7.17 |
| CHEMBL3402573 | — | — | 1 | 7.16 |
| CHEMBL3400975 | — | — | 1 | 7.13 |
| CHEMBL3402579 | — | — | 1 | 7.11 |
| CHEMBL3400974 | — | — | 1 | 7.04 |
| CHEMBL3402574 | — | — | 1 | 6.92 |
| CHEMBL3400977 | — | — | 1 | 6.87 |
| CHEMBL3402577 | — | — | 1 | 6.71 |
| CHEMBL3402590 | — | — | 1 | 6.24 |
| CHEMBL3402578 | — | — | 1 | 5.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3402585 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3402584 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2057918 | — | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL3402583 | — | IC50 | = | 15.3 | nM | 7.82 |
| CHEMBL3400174 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL3402587 | — | IC50 | = | 16.5 | nM | 7.78 |
| CHEMBL3400979 | — | IC50 | = | 17.8 | nM | 7.75 |
| CHEMBL3402569 | — | IC50 | = | 18.2 | nM | 7.74 |
| CHEMBL3402576 | — | IC50 | = | 21.3 | nM | 7.67 |
| CHEMBL3402588 | — | IC50 | = | 24.8 | nM | 7.61 |
| CHEMBL3402586 | — | IC50 | = | 25.2 | nM | 7.60 |
| CHEMBL3402571 | — | IC50 | = | 31.6 | nM | 7.50 |
| CHEMBL3402581 | — | IC50 | = | 32.5 | nM | 7.49 |
| CHEMBL3402575 | — | IC50 | = | 38.8 | nM | 7.41 |
| CHEMBL3400978 | — | IC50 | = | 41.7 | nM | 7.38 |
| CHEMBL3402589 | — | IC50 | = | 45.3 | nM | 7.34 |
| CHEMBL3402570 | — | IC50 | = | 50.8 | nM | 7.29 |
| CHEMBL3402582 | — | IC50 | = | 57.1 | nM | 7.24 |
| CHEMBL3400976 | — | IC50 | = | 58.3 | nM | 7.23 |
| CHEMBL3402572 | — | IC50 | = | 63.6 | nM | 7.20 |
| CHEMBL3402580 | — | IC50 | = | 67.1 | nM | 7.17 |
| CHEMBL3402573 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL3400975 | — | IC50 | = | 73.9 | nM | 7.13 |
| CHEMBL3402579 | — | IC50 | = | 77.8 | nM | 7.11 |
| CHEMBL3400974 | — | IC50 | = | 90.3 | nM | 7.04 |
| CHEMBL3402574 | — | IC50 | = | 118.8 | nM | 6.92 |
| CHEMBL3400977 | — | IC50 | = | 135.5 | nM | 6.87 |
| CHEMBL3402577 | — | IC50 | = | 197.4 | nM | 6.71 |
| CHEMBL3402590 | — | IC50 | = | 574.0 | nM | 6.24 |
| CHEMBL3402578 | — | IC50 | = | 1357.0 | nM | 5.87 |
| CHEMBL3400973 | — | IC50 | = | 1568.0 | nM | 5.80 |
| CHEMBL3402591 | — | IC50 | > | 5000.0 | nM | - |