Assay Detail
Functional
CHEMBL863867
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TCR stimulated IL2 production in mice administered orally
18
Total Activities
16
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Proto-oncogene tyrosine-protein kinase LCK (CHEMBL2480) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| ED50 | 15 | - | - |
| ED90 | 2 | - | - |
| EC50 | 1 | 7.11 | 7.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL197603 | — | — | 1 | 7.11 |
| CHEMBL200587 | — | — | 1 | - |
| CHEMBL199813 | — | — | 1 | - |
| CHEMBL370670 | — | — | 1 | - |
| CHEMBL200424 | — | — | 1 | - |
| CHEMBL199816 | — | — | 1 | - |
| CHEMBL440213 | — | — | 1 | - |
| CHEMBL381203 | — | — | 2 | - |
| CHEMBL199369 | — | — | 1 | - |
| CHEMBL371459 | — | — | 1 | - |
| CHEMBL371295 | — | — | 1 | - |
| CHEMBL198239 | — | — | 1 | - |
| CHEMBL373054 | — | — | 1 | - |
| CHEMBL198136 | — | — | 1 | - |
| CHEMBL370383 | — | — | 1 | - |
| CHEMBL370773 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL197603 | — | EC50 | = | 78.0 | nM | 7.11 |
| CHEMBL200587 | — | ED50 | = | 27.0 | mg.kg-1 | - |
| CHEMBL199813 | — | ED50 | - | — | - | |
| CHEMBL370670 | — | ED50 | - | — | - | |
| CHEMBL200424 | — | ED50 | - | — | - | |
| CHEMBL199816 | — | ED50 | - | — | - | |
| CHEMBL440213 | — | ED50 | - | — | - | |
| CHEMBL381203 | — | ED50 | = | 1.8 | mg.kg-1 | - |
| CHEMBL199369 | — | ED50 | = | 17.9 | mg.kg-1 | - |
| CHEMBL371459 | — | ED50 | = | 9.2 | mg.kg-1 | - |
| CHEMBL198239 | — | ED50 | = | 7.0 | mg.kg-1 | - |
| CHEMBL373054 | — | ED50 | - | — | - | |
| CHEMBL198136 | — | ED50 | = | 17.8 | mg.kg-1 | - |
| CHEMBL370383 | — | ED50 | - | — | - | |
| CHEMBL370773 | — | ED50 | = | 3.6 | mg.kg-1 | - |
| CHEMBL381203 | — | ED90 | = | 15.5 | mg kg-1 | - |
| CHEMBL370773 | — | ED90 | = | 19.0 | mg kg-1 | - |
| CHEMBL371295 | — | ED50 | - | — | - |