Assay Detail
Binding
CHEMBL678141
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Inhibitory binding activity against human Immunophilin-FK-506 binding protein 12
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Peptidyl-prolyl cis-trans isomerase FKBP1A (CHEMBL1902) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
32-Ascomycinyloxyacetic acid derived immunosuppressants. Independence of immunophilin binding and immunosuppressive potency.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.82 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL262778 | — | — | 1 | 9.40 |
| CHEMBL52035 | — | — | 1 | 9.22 |
| CHEMBL413 | SIROLIMUS | 4.0 | 1 | 8.96 |
| CHEMBL48863 | — | — | 1 | 8.70 |
| CHEMBL8597 | ASCOMYCIN | — | 1 | 8.68 |
| CHEMBL263776 | — | — | 1 | 8.62 |
| CHEMBL269732 | TACROLIMUS ANHYDROUS | 4.0 | 1 | 8.60 |
| CHEMBL299136 | — | — | 1 | 8.54 |
| CHEMBL295372 | — | — | 1 | 8.49 |
| CHEMBL432484 | — | — | 1 | 8.48 |
| CHEMBL51516 | — | — | 1 | 8.40 |
| CHEMBL266912 | — | — | 1 | 8.25 |
| CHEMBL299146 | — | — | 1 | 8.03 |
| CHEMBL264789 | — | — | 1 | 7.89 |
| CHEMBL52055 | — | — | 1 | 7.80 |
| CHEMBL385686 | — | — | 1 | 7.72 |
| CHEMBL51334 | — | — | 1 | 7.34 |
| CHEMBL51523 | — | — | 1 | 7.32 |
| CHEMBL266263 | — | — | 1 | 7.30 |
| CHEMBL296160 | — | — | 1 | 7.17 |
| CHEMBL295945 | — | — | 1 | 7.15 |
| CHEMBL51424 | — | — | 1 | 6.77 |
| CHEMBL48841 | — | — | 1 | 6.75 |
| CHEMBL299549 | — | — | 1 | 6.75 |
| CHEMBL262844 | — | — | 1 | 6.33 |
| CHEMBL411841 | — | — | 1 | 6.30 |
| CHEMBL274090 | — | — | 1 | 6.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL262778 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL52035 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL413 | SIROLIMUS | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL48863 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL8597 | ASCOMYCIN | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL263776 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL269732 | TACROLIMUS ANHYDROUS | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL299136 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL295372 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL432484 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL51516 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL266912 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL299146 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL264789 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL52055 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL385686 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL51334 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL51523 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL266263 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL296160 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL295945 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL51424 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL48841 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL299549 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL262844 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL411841 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL274090 | — | IC50 | = | 570.0 | nM | 6.24 |