Assay Detail
Functional
CHEMBL812192
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonistic activity in a murine splenic T-cell proliferation assay was calculated by measurement of [3H]thymidine uptake relative to control
24
Total Activities
24
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 | Expert |
Publication
Novel derivatives at the C21 position of the FK-506 macrocycle
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 7.04 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL269732 | TACROLIMUS ANHYDROUS | 4.0 | 1 | 9.74 |
| CHEMBL8597 | ASCOMYCIN | — | 1 | 9.16 |
| CHEMBL347139 | — | — | 1 | 9.03 |
| CHEMBL422367 | — | — | 1 | 8.67 |
| CHEMBL352172 | — | — | 1 | 8.58 |
| CHEMBL351445 | — | — | 1 | 8.56 |
| CHEMBL351140 | — | — | 1 | 8.30 |
| CHEMBL348352 | — | — | 1 | 8.15 |
| CHEMBL158960 | — | — | 1 | 7.77 |
| CHEMBL346057 | — | — | 1 | 7.77 |
| CHEMBL436659 | — | — | 1 | 7.69 |
| CHEMBL422171 | — | — | 1 | 7.00 |
| CHEMBL349585 | — | — | 1 | 5.93 |
| CHEMBL347589 | — | — | 1 | 5.88 |
| CHEMBL347657 | — | — | 1 | 5.78 |
| CHEMBL158921 | — | — | 1 | 5.68 |
| CHEMBL347383 | — | — | 1 | 5.47 |
| CHEMBL161316 | — | — | 1 | 5.44 |
| CHEMBL162354 | — | — | 1 | 5.37 |
| CHEMBL350884 | — | — | 1 | 5.00 |
| CHEMBL161068 | — | — | 1 | 4.94 |
| CHEMBL348122 | — | — | 1 | 4.93 |
| CHEMBL423774 | — | — | 1 | - |
| CHEMBL407238 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL269732 | TACROLIMUS ANHYDROUS | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL8597 | ASCOMYCIN | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL347139 | — | IC50 | = | 0.93 | nM | 9.03 |
| CHEMBL422367 | — | IC50 | = | 2.14 | nM | 8.67 |
| CHEMBL352172 | — | IC50 | = | 2.62 | nM | 8.58 |
| CHEMBL351445 | — | IC50 | = | 2.72 | nM | 8.56 |
| CHEMBL351140 | — | IC50 | = | 4.98 | nM | 8.30 |
| CHEMBL348352 | — | IC50 | = | 7.12 | nM | 8.15 |
| CHEMBL158960 | — | IC50 | = | 16.9 | nM | 7.77 |
| CHEMBL346057 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL436659 | — | IC50 | = | 20.5 | nM | 7.69 |
| CHEMBL422171 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL349585 | — | IC50 | = | 1182.0 | nM | 5.93 |
| CHEMBL347589 | — | IC50 | = | 1327.0 | nM | 5.88 |
| CHEMBL347657 | — | IC50 | = | 1677.0 | nM | 5.78 |
| CHEMBL158921 | — | IC50 | = | 2087.0 | nM | 5.68 |
| CHEMBL347383 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL161316 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL162354 | — | IC50 | = | 4248.0 | nM | 5.37 |
| CHEMBL350884 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL161068 | — | IC50 | = | 11400.0 | nM | 4.94 |
| CHEMBL348122 | — | IC50 | = | 11800.0 | nM | 4.93 |
| CHEMBL423774 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL407238 | — | IC50 | - | nM | - |