Assay Detail
Binding
CHEMBL678158
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In vitro competitive binding to FK506 binding protein 12 versus tritiated FK-506.
8
Total Activities
8
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
Preparation and in vitro activities of naphthyl and indolyl ether derivatives of the FK-506 related immunosuppressive macrolide ascomycin
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 8.43 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL303852 | — | — | 1 | 9.15 |
| CHEMBL68027 | — | — | 1 | 9.10 |
| CHEMBL70822 | — | — | 1 | 8.80 |
| CHEMBL303180 | — | — | 1 | 8.55 |
| CHEMBL419817 | — | — | 1 | 8.44 |
| CHEMBL431360 | — | — | 1 | 8.29 |
| CHEMBL71849 | — | — | 1 | 8.00 |
| CHEMBL302040 | — | — | 1 | 7.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL303852 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL68027 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL70822 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL303180 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL419817 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL431360 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL71849 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL302040 | — | IC50 | = | 74.8 | nM | 7.13 |