Assay Detail
Binding
CHEMBL678154
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Binding affinity for FK506 binding protein 12 using [3H]-dihydro FK-506 radioligand was determined
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Peptidyl-prolyl cis-trans isomerase FKBP1A (CHEMBL1902) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
C32-O-imidazol-2-yl-methyl ether derivatives of the immunosuppressant ascomycin with improved therapeutic potential.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 8.01 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL8597 | ASCOMYCIN | — | 1 | 8.80 |
| CHEMBL386482 | — | — | 1 | 8.13 |
| CHEMBL385568 | — | — | 1 | 7.92 |
| CHEMBL428499 | — | — | 1 | 7.66 |
| CHEMBL262667 | — | — | 1 | 7.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL8597 | ASCOMYCIN | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL386482 | — | EC50 | = | 7.4 | nM | 8.13 |
| CHEMBL385568 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL428499 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL262667 | — | EC50 | = | 30.0 | nM | 7.52 |