Assay Detail
Binding
CHEMBL4189646
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human BTK using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA
27
Total Activities
27
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 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 8.25 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4211949 | — | — | 1 | 9.40 |
| CHEMBL4214532 | — | — | 1 | 9.40 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 9.40 |
| CHEMBL4206284 | — | — | 1 | 9.30 |
| CHEMBL4202814 | — | — | 1 | 9.10 |
| CHEMBL4209773 | — | — | 1 | 8.68 |
| CHEMBL4217114 | — | — | 1 | 8.66 |
| CHEMBL4214872 | — | — | 1 | 8.55 |
| CHEMBL4217006 | — | — | 1 | 8.55 |
| CHEMBL4211579 | — | — | 1 | 8.52 |
| CHEMBL4208616 | — | — | 1 | 8.51 |
| CHEMBL4215249 | — | — | 1 | 8.48 |
| CHEMBL4203064 | — | — | 1 | 8.46 |
| CHEMBL4217820 | — | — | 1 | 8.43 |
| CHEMBL4203739 | — | — | 1 | 8.37 |
| CHEMBL4203826 | — | — | 1 | 8.37 |
| CHEMBL4209342 | — | — | 1 | 8.28 |
| CHEMBL4214492 | — | — | 1 | 8.21 |
| CHEMBL4203756 | — | — | 1 | 8.13 |
| CHEMBL4204398 | — | — | 1 | 7.63 |
| CHEMBL4215470 | — | — | 1 | 7.62 |
| CHEMBL4216788 | — | — | 1 | 7.40 |
| CHEMBL4207689 | — | — | 1 | 7.30 |
| CHEMBL4217471 | — | — | 1 | 7.20 |
| CHEMBL4209048 | — | — | 1 | 6.38 |
| CHEMBL4218760 | — | — | 1 | 6.14 |
| CHEMBL4204932 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4211949 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4214532 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4206284 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4202814 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4209773 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4217114 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4214872 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4217006 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4211579 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4208616 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4215249 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4203064 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4217820 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4203739 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4203826 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4209342 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4214492 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4203756 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL4204398 | — | IC50 | = | 23.6 | nM | 7.63 |
| CHEMBL4215470 | — | IC50 | = | 23.8 | nM | 7.62 |
| CHEMBL4216788 | — | IC50 | = | 40.1 | nM | 7.40 |
| CHEMBL4207689 | — | IC50 | = | 50.4 | nM | 7.30 |
| CHEMBL4217471 | — | IC50 | = | 62.6 | nM | 7.20 |
| CHEMBL4209048 | — | IC50 | = | 417.4 | nM | 6.38 |
| CHEMBL4218760 | — | IC50 | = | 725.2 | nM | 6.14 |
| CHEMBL4204932 | — | IC50 | > | 1000.0 | nM | - |