Assay Detail
Binding
CHEMBL678139
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Effective concentration against FK506 binding protein 12 using [3H]-dihydro FK-506
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Peptidyl-prolyl cis-trans isomerase FKBP1A (CHEMBL1902) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Potent immunosuppressive C32-O-arylethyl ether derivatives of ascomycin with reduced toxicity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 7.93 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL269732 | TACROLIMUS ANHYDROUS | 4.0 | 1 | 9.05 |
| CHEMBL275103 | — | — | 1 | 8.12 |
| CHEMBL65863 | — | — | 1 | 8.12 |
| CHEMBL305081 | — | — | 1 | 8.05 |
| CHEMBL266705 | — | — | 1 | 7.95 |
| CHEMBL268110 | — | — | 1 | 7.92 |
| CHEMBL431368 | — | — | 1 | 7.87 |
| CHEMBL264568 | — | — | 1 | 7.75 |
| CHEMBL407332 | — | — | 1 | 7.68 |
| CHEMBL412791 | — | — | 1 | 7.35 |
| CHEMBL405917 | — | — | 1 | 7.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL269732 | TACROLIMUS ANHYDROUS | EC50 | = | 0.9 | nM | 9.05 |
| CHEMBL275103 | — | EC50 | = | 7.5 | nM | 8.12 |
| CHEMBL65863 | — | EC50 | = | 7.5 | nM | 8.12 |
| CHEMBL305081 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL266705 | — | EC50 | = | 11.25 | nM | 7.95 |
| CHEMBL268110 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL431368 | — | EC50 | = | 13.6 | nM | 7.87 |
| CHEMBL264568 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL407332 | — | EC50 | = | 21.1 | nM | 7.68 |
| CHEMBL412791 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL405917 | — | EC50 | = | 45.0 | nM | 7.35 |