Assay Detail
Binding
CHEMBL4835124
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of fluorescent tracer 5-(3-(4-((1S,5S,6S)-10-(3,5-dichlorophenylsulfonyl)-2-oxo-3-(pyridin-3-ylmethyl)-3,10-diazabicyclo[4.3.1]decan-5-yl)-1H-1,2,3-triazol-1-yl)propylcarbamoyl)-2-(6-(dimethylamino)-3-(dimethyliminio)-3H-xanthen-9-yl)benzoate from recombinant full length C-terminal FLAG-tagged FKBP52 (unknown origin) expressed in Escherichia coli BL21 (DE3) cells incubated for 30 mins by fluorescence polarisation competition binding assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peptidyl-prolyl cis-trans isomerase FKBP4 (CHEMBL4050) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-Based Design of High-Affinity Macrocyclic FKBP51 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 34 | 5.48 | 6.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4871144 | — | — | 1 | 6.29 |
| CHEMBL4856956 | — | — | 1 | 6.10 |
| CHEMBL4858532 | — | — | 1 | 5.85 |
| CHEMBL4863989 | — | — | 1 | 5.45 |
| CHEMBL4866742 | — | — | 1 | 5.41 |
| CHEMBL4878667 | — | — | 1 | 5.41 |
| CHEMBL4876415 | — | — | 1 | 5.39 |
| CHEMBL4872580 | — | — | 1 | 5.35 |
| CHEMBL4878890 | — | — | 1 | 5.33 |
| CHEMBL4868302 | — | — | 1 | 5.27 |
| CHEMBL4859741 | — | — | 1 | 5.04 |
| CHEMBL4879078 | — | — | 1 | 4.88 |
| CHEMBL4863807 | — | — | 1 | - |
| CHEMBL4867024 | — | — | 1 | - |
| CHEMBL4863883 | — | — | 1 | - |
| CHEMBL4863758 | — | — | 1 | - |
| CHEMBL4866065 | — | — | 1 | - |
| CHEMBL4860544 | — | — | 1 | - |
| CHEMBL4874574 | — | — | 1 | - |
| CHEMBL4855135 | — | — | 1 | - |
| CHEMBL4853042 | — | — | 1 | - |
| CHEMBL4856203 | — | — | 1 | - |
| CHEMBL4862808 | — | — | 1 | - |
| CHEMBL4877731 | — | — | 1 | - |
| CHEMBL4870008 | — | — | 1 | - |
| CHEMBL4862282 | — | — | 1 | - |
| CHEMBL4864747 | — | — | 1 | - |
| CHEMBL4876664 | — | — | 1 | - |
| CHEMBL4850750 | — | — | 1 | - |
| CHEMBL4850434 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4871144 | — | Kd | = | 513.0 | nM | 6.29 |
| CHEMBL4856956 | — | Kd | = | 795.0 | nM | 6.10 |
| CHEMBL4858532 | — | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL4863989 | — | Kd | = | 3529.0 | nM | 5.45 |
| CHEMBL4866742 | — | Kd | = | 3877.0 | nM | 5.41 |
| CHEMBL4878667 | — | Kd | = | 3855.0 | nM | 5.41 |
| CHEMBL4876415 | — | Kd | = | 4098.0 | nM | 5.39 |
| CHEMBL4872580 | — | Kd | = | 4459.0 | nM | 5.35 |
| CHEMBL4878890 | — | Kd | = | 4671.0 | nM | 5.33 |
| CHEMBL4868302 | — | Kd | = | 5395.0 | nM | 5.27 |
| CHEMBL4859741 | — | Kd | = | 9088.0 | nM | 5.04 |
| CHEMBL4879078 | — | Kd | = | 13199.0 | nM | 4.88 |
| CHEMBL4856457 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4848201 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4875870 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4872122 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4863807 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4867024 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4863883 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4863758 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4866065 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4860544 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4874574 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4855135 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4853042 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4856203 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4862808 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4877731 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4870008 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4862282 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4864747 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4876664 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4850750 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4850434 | — | Kd | > | 10000.0 | nM | - |