Assay Detail
Binding
CHEMBL4258267
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human FKBP12 expressed in Escherichia coli using succinyl-Ala-Phe-Pro-Phe-4-nitroanilide as substrate measured after 5 to 10 mins by spectrophotometric method
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peptidyl-prolyl cis-trans isomerase FKBP1A (CHEMBL1902) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological evaluation of rapamycin-derived, next generation small molecules.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 8.45 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL413 | SIROLIMUS | 4.0 | 1 | 9.22 |
| CHEMBL4276944 | — | — | 1 | 9.00 |
| CHEMBL4291053 | — | — | 1 | 9.00 |
| CHEMBL4287849 | — | — | 1 | 9.00 |
| CHEMBL4291011 | — | — | 1 | 9.00 |
| CHEMBL4280369 | — | — | 1 | 9.00 |
| CHEMBL4279943 | — | — | 1 | 8.82 |
| CHEMBL4281041 | — | — | 1 | 8.52 |
| CHEMBL4287588 | — | — | 1 | 8.46 |
| CHEMBL216404 | — | — | 1 | 8.43 |
| CHEMBL4283828 | — | — | 1 | 8.35 |
| CHEMBL4279511 | — | — | 1 | 8.30 |
| CHEMBL4283415 | — | — | 1 | 8.22 |
| CHEMBL4291680 | — | — | 1 | 8.15 |
| CHEMBL4280419 | — | — | 1 | 8.15 |
| CHEMBL4295102 | — | — | 1 | 8.05 |
| CHEMBL4291252 | — | — | 1 | 8.00 |
| CHEMBL4290182 | — | — | 1 | 7.54 |
| CHEMBL4284445 | — | — | 1 | 7.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL413 | SIROLIMUS | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL4276944 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4291053 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4287849 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4291011 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4280369 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4279943 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL4281041 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4287588 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL216404 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL4283828 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL4279511 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL4283415 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4291680 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL4280419 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL4295102 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL4291252 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4290182 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL4284445 | — | Ki | = | 38.0 | nM | 7.42 |