Assay Detail
Binding
CHEMBL678151
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Ability to bind the major cystolic receptor FK506 binding protein 12 by using competitive binding assay
16
Total Activities
16
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
Alkyl ether derivatives of the FK-506 related, immunosuppressive macrolide L-683,742 (C31-O-desmethyl ascomycin)
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 8.17 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL8597 | ASCOMYCIN | — | 1 | 8.80 |
| CHEMBL170544 | — | — | 1 | 8.57 |
| CHEMBL368142 | — | — | 1 | 8.34 |
| CHEMBL2062149 | — | — | 1 | 8.30 |
| CHEMBL435906 | — | — | 1 | 8.24 |
| CHEMBL170655 | — | — | 1 | 8.21 |
| CHEMBL355620 | — | — | 1 | 8.18 |
| CHEMBL366891 | — | — | 1 | 8.15 |
| CHEMBL369579 | — | — | 1 | 8.04 |
| CHEMBL433606 | — | — | 1 | 7.99 |
| CHEMBL439899 | — | — | 1 | 7.93 |
| CHEMBL366353 | — | — | 1 | 7.92 |
| CHEMBL174029 | — | — | 1 | 7.83 |
| CHEMBL176774 | — | — | 1 | 7.81 |
| CHEMBL407020 | — | — | 1 | - |
| CHEMBL173862 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL8597 | ASCOMYCIN | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL170544 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL368142 | — | EC50 | = | 4.6 | nM | 8.34 |
| CHEMBL2062149 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL435906 | — | EC50 | = | 5.7 | nM | 8.24 |
| CHEMBL170655 | — | EC50 | = | 6.1 | nM | 8.21 |
| CHEMBL355620 | — | EC50 | = | 6.6 | nM | 8.18 |
| CHEMBL366891 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL369579 | — | EC50 | = | 9.2 | nM | 8.04 |
| CHEMBL433606 | — | EC50 | = | 10.3 | nM | 7.99 |
| CHEMBL439899 | — | EC50 | = | 11.8 | nM | 7.93 |
| CHEMBL366353 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL174029 | — | EC50 | = | 14.9 | nM | 7.83 |
| CHEMBL176774 | — | EC50 | = | 15.6 | nM | 7.81 |
| CHEMBL407020 | — | EC50 | - | nM | - | |
| CHEMBL173862 | — | EC50 | - | nM | - |