Assay Detail
Binding
CHEMBL4178244
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Inhibition of recombinant human full length BTK preincubated for 10 mins followed by Tk-biotin peptide substrate addition after 90 mins by TR-FRET assay
18
Total Activities
18
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 and evaluation of 1H-pyrrolo[2,3-b]pyridine based selective and reversible small molecule BTK inhibitors for the treatment of rheumatoid arthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 8.46 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3928203 | — | — | 1 | 9.00 |
| CHEMBL3936823 | — | — | 1 | 9.00 |
| CHEMBL3982806 | — | — | 1 | 8.96 |
| CHEMBL4216939 | — | — | 1 | 8.92 |
| CHEMBL3946460 | — | — | 1 | 8.85 |
| CHEMBL3959033 | — | — | 1 | 8.77 |
| CHEMBL3967108 | — | — | 1 | 8.59 |
| CHEMBL3900184 | — | — | 1 | 8.59 |
| CHEMBL3966346 | — | — | 1 | 8.51 |
| CHEMBL3962146 | — | — | 1 | 8.29 |
| CHEMBL3922230 | — | — | 1 | 8.27 |
| CHEMBL3891434 | — | — | 1 | 8.26 |
| CHEMBL3891185 | — | — | 1 | 8.22 |
| CHEMBL3921350 | — | — | 1 | 8.19 |
| CHEMBL3907763 | — | — | 1 | 8.17 |
| CHEMBL3935716 | — | — | 1 | 8.08 |
| CHEMBL3968892 | — | — | 1 | 7.93 |
| CHEMBL3968928 | — | — | 1 | 7.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3928203 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3936823 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3982806 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4216939 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3946460 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3959033 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3967108 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3900184 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3966346 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3962146 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3922230 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL3891434 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3891185 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3921350 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL3907763 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL3935716 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL3968892 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL3968928 | — | IC50 | = | 21.0 | nM | 7.68 |