Assay Detail
Binding
CHEMBL4235696
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human full-length His-tagged BTK cytoplasmic domain expressed in baculovirus expression system using fluorescence-labelled peptide as substrate measured after 60 mins by fluorescence assay
34
Total Activities
34
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
Conversion of carbazole carboxamide based reversible inhibitors of Bruton's tyrosine kinase (BTK) into potent, selective irreversible inhibitors in the carbazole, tetrahydrocarbazole, and a new 2,3-dimethylindole series.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 8.88 | 10.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4237999 | — | — | 1 | 10.17 |
| CHEMBL4242527 | — | — | 1 | 10.11 |
| CHEMBL4240879 | — | — | 1 | 10.10 |
| CHEMBL4246324 | — | — | 1 | 9.96 |
| CHEMBL4248386 | — | — | 1 | 9.85 |
| CHEMBL4248271 | — | — | 1 | 9.80 |
| CHEMBL4248719 | — | — | 1 | 9.77 |
| CHEMBL4248550 | — | — | 1 | 9.74 |
| CHEMBL4243995 | — | — | 1 | 9.68 |
| CHEMBL4241958 | — | — | 1 | 9.68 |
| CHEMBL4247992 | — | — | 1 | 9.64 |
| CHEMBL4237249 | — | — | 1 | 9.62 |
| CHEMBL4238798 | — | — | 1 | 9.49 |
| CHEMBL4237557 | — | — | 1 | 9.42 |
| CHEMBL4239747 | — | — | 1 | 9.34 |
| CHEMBL4242058 | — | — | 1 | 9.23 |
| CHEMBL4238297 | — | — | 1 | 9.09 |
| CHEMBL4248834 | — | — | 1 | 8.96 |
| CHEMBL4239031 | — | — | 1 | 8.96 |
| CHEMBL4245037 | — | — | 1 | 8.92 |
| CHEMBL4246005 | — | — | 1 | 8.92 |
| CHEMBL4251151 | — | — | 1 | 8.62 |
| CHEMBL3918580 | — | — | 1 | 8.59 |
| CHEMBL4249247 | — | — | 1 | 8.46 |
| CHEMBL4238256 | — | — | 1 | 8.14 |
| CHEMBL4244928 | — | — | 1 | 8.04 |
| CHEMBL4237800 | — | — | 1 | 8.03 |
| CHEMBL4240731 | — | — | 1 | 7.92 |
| CHEMBL4241723 | — | — | 1 | 7.92 |
| CHEMBL4243299 | — | — | 1 | 7.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4237999 | — | IC50 | = | 0.068 | nM | 10.17 |
| CHEMBL4242527 | — | IC50 | = | 0.077 | nM | 10.11 |
| CHEMBL4240879 | — | IC50 | = | 0.079 | nM | 10.10 |
| CHEMBL4246324 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL4248386 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL4248271 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL4248719 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL4248550 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL4243995 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL4241958 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL4247992 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL4237249 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL4238798 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL4237557 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL4239747 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL4242058 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL4238297 | — | IC50 | = | 0.82 | nM | 9.09 |
| CHEMBL4248834 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4239031 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4245037 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4246005 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4251151 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3918580 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4249247 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4238256 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL4244928 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL4237800 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL4240731 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4241723 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4243299 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4238212 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4237436 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4249677 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4245876 | — | IC50 | = | 550.0 | nM | 6.26 |