Assay Detail
Binding
CHEMBL5524495
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Inhibition of GST-tagged human FKBP52 expressed in Escherichia coli BL21 (DE3) using NH2-EDASRMEEVD-COOH peptide as substrate preincubated for 15 mins followed by substrate addition measured after 15 mins by Alpha Screen assay
13
Total Activities
13
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 FKBP4 (CHEMBL4050) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-based discovery of small molecule inhibitors of FKBP51-Hsp90 protein-protein interaction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.32 | 5.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5558644 | — | — | 1 | 5.52 |
| CHEMBL5556796 | — | — | 1 | 5.52 |
| CHEMBL5555524 | — | — | 1 | 5.52 |
| CHEMBL1322226 | — | — | 1 | 5.52 |
| CHEMBL5558181 | — | — | 1 | 5.30 |
| CHEMBL5568553 | — | — | 1 | 5.30 |
| CHEMBL5565884 | — | — | 1 | 5.30 |
| CHEMBL5567729 | — | — | 1 | 5.22 |
| CHEMBL5562308 | — | — | 1 | 5.22 |
| CHEMBL5564982 | — | — | 1 | 5.22 |
| CHEMBL1463946 | — | — | 1 | 5.10 |
| CHEMBL5561271 | — | — | 1 | 5.05 |
| CHEMBL5563469 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5558644 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5556796 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5555524 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1322226 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5558181 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5568553 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5565884 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5567729 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL5562308 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL5564982 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL1463946 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL5561271 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL5563469 | — | IC50 | > | 100000.0 | nM | - |