Assay Detail
Binding
CHEMBL4258268
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FKBP12 in mouse T cells assessed as reduction in cell proliferation
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Peptidyl-prolyl cis-trans isomerase FKBP1A (CHEMBL4295736) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Synthesis and biological evaluation of rapamycin-derived, next generation small molecules.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.60 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL413 | SIROLIMUS | 4.0 | 1 | 9.00 |
| CHEMBL4287849 | — | — | 1 | 8.70 |
| CHEMBL4280369 | — | — | 1 | 8.40 |
| CHEMBL4291011 | — | — | 1 | 8.40 |
| CHEMBL4279511 | — | — | 1 | 8.22 |
| CHEMBL4287588 | — | — | 1 | 8.00 |
| CHEMBL4291252 | — | — | 1 | 7.96 |
| CHEMBL4283415 | — | — | 1 | 7.70 |
| CHEMBL4281041 | — | — | 1 | 7.70 |
| CHEMBL4276944 | — | — | 1 | 7.52 |
| CHEMBL4291053 | — | — | 1 | 7.35 |
| CHEMBL4280419 | — | — | 1 | 7.30 |
| CHEMBL4279943 | — | — | 1 | 7.16 |
| CHEMBL4290182 | — | — | 1 | 6.52 |
| CHEMBL4295102 | — | — | 1 | 6.00 |
| CHEMBL216404 | — | — | 1 | 5.60 |
| CHEMBL4291680 | — | — | 1 | - |
| CHEMBL4284445 | — | — | 1 | - |
| CHEMBL4283828 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL413 | SIROLIMUS | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4287849 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4280369 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4291011 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4279511 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4287588 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4291252 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4283415 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4281041 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4276944 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4291053 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4280419 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4279943 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4290182 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4295102 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL216404 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4291680 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4284445 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4283828 | — | IC50 | > | 10000.0 | nM | - |