Assay Detail
Functional
CHEMBL812190
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Concentration required to reverse inhibition of T-cell proliferation, by measuring [3H]thymidine uptake up to a concentration of 10 uM (Antagonistic activity, immunosuppression)
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | T-cell |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Novel derivatives at the C21 position of the FK-506 macrocycle
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 6.75 | 7.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL347589 | — | — | 1 | 7.93 |
| CHEMBL349585 | — | — | 1 | 7.47 |
| CHEMBL423774 | — | — | 1 | 7.29 |
| CHEMBL407238 | — | — | 1 | 7.19 |
| CHEMBL348122 | — | — | 1 | 7.06 |
| CHEMBL161068 | — | — | 1 | 6.67 |
| CHEMBL350884 | — | — | 1 | 6.64 |
| CHEMBL422171 | — | — | 1 | 6.00 |
| CHEMBL161316 | — | — | 1 | 5.75 |
| CHEMBL162354 | — | — | 1 | 5.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL347589 | — | EC50 | = | 11.8 | nM | 7.93 |
| CHEMBL349585 | — | EC50 | = | 34.1 | nM | 7.47 |
| CHEMBL423774 | — | EC50 | = | 51.0 | nM | 7.29 |
| CHEMBL407238 | — | EC50 | = | 64.0 | nM | 7.19 |
| CHEMBL348122 | — | EC50 | = | 88.0 | nM | 7.06 |
| CHEMBL161068 | — | EC50 | = | 212.0 | nM | 6.67 |
| CHEMBL350884 | — | EC50 | = | 228.0 | nM | 6.64 |
| CHEMBL422171 | — | EC50 | = | 992.0 | nM | 6.00 |
| CHEMBL161316 | — | EC50 | = | 1780.0 | nM | 5.75 |
| CHEMBL162354 | — | EC50 | = | 3522.0 | nM | 5.45 |