Assay Detail
ADMET
CHEMBL4385482
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full-length recombinant human C-terminal His-tagged SRC cytoplasmic domain expressed in baculovirus expression system using FAM-Srctide peptide as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by TR-FRET Lanthascreen assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Proto-oncogene tyrosine-protein kinase Src (CHEMBL267) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.96 | 8.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4436118 | — | — | 1 | 8.38 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 7.42 |
| CHEMBL4520801 | — | — | 1 | 7.14 |
| CHEMBL4572913 | — | — | 1 | 6.43 |
| CHEMBL4456283 | — | — | 1 | 5.85 |
| CHEMBL4560385 | — | — | 1 | 5.79 |
| CHEMBL4556666 | — | — | 1 | 5.50 |
| CHEMBL4548556 | — | — | 1 | 5.47 |
| CHEMBL4518667 | — | — | 1 | 5.47 |
| CHEMBL4442732 | — | — | 1 | 5.39 |
| CHEMBL4440096 | — | — | 1 | 5.34 |
| CHEMBL4559065 | — | — | 1 | 5.23 |
| CHEMBL4591391 | — | — | 1 | 5.19 |
| CHEMBL4456974 | — | — | 1 | 4.84 |
| CHEMBL4462332 | — | — | 1 | - |
| CHEMBL4469663 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4436118 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4520801 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4572913 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4456283 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4560385 | — | IC50 | = | 1630.0 | nM | 5.79 |
| CHEMBL4556666 | — | IC50 | = | 3140.0 | nM | 5.50 |
| CHEMBL4548556 | — | IC50 | = | 3410.0 | nM | 5.47 |
| CHEMBL4518667 | — | IC50 | = | 3350.0 | nM | 5.47 |
| CHEMBL4442732 | — | IC50 | = | 4030.0 | nM | 5.39 |
| CHEMBL4440096 | — | IC50 | = | 4610.0 | nM | 5.34 |
| CHEMBL4559065 | — | IC50 | = | 5840.0 | nM | 5.23 |
| CHEMBL4591391 | — | IC50 | = | 6480.0 | nM | 5.19 |
| CHEMBL4456974 | — | IC50 | = | 14400.0 | nM | 4.84 |
| CHEMBL4462332 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4469663 | — | IC50 | > | 20000.0 | nM | - |