Assay Detail
Binding
CHEMBL4835126
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 FKBP12 (unknown origin) expressed in Escherichia coli BL21 (DE2) 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 FKBP1A (CHEMBL1902) ↗| 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 | 6.59 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4871144 | — | — | 1 | 7.66 |
| CHEMBL4858532 | — | — | 1 | 7.42 |
| CHEMBL4878667 | — | — | 1 | 7.36 |
| CHEMBL4863989 | — | — | 1 | 7.23 |
| CHEMBL4866742 | — | — | 1 | 7.21 |
| CHEMBL4876415 | — | — | 1 | 7.18 |
| CHEMBL4856956 | — | — | 1 | 7.10 |
| CHEMBL4878890 | — | — | 1 | 7.07 |
| CHEMBL4872580 | — | — | 1 | 6.95 |
| CHEMBL4870008 | — | — | 1 | 6.90 |
| CHEMBL4862282 | — | — | 1 | 6.87 |
| CHEMBL4850434 | — | — | 1 | 6.86 |
| CHEMBL4862808 | — | — | 1 | 6.72 |
| CHEMBL4868302 | — | — | 1 | 6.67 |
| CHEMBL4859741 | — | — | 1 | 6.61 |
| CHEMBL4876664 | — | — | 1 | 6.58 |
| CHEMBL4879078 | — | — | 1 | 6.53 |
| CHEMBL4856203 | — | — | 1 | 6.46 |
| CHEMBL4850750 | — | — | 1 | 6.45 |
| CHEMBL4853042 | — | — | 1 | 6.32 |
| CHEMBL4877731 | — | — | 1 | 6.31 |
| CHEMBL4863883 | — | — | 1 | 6.28 |
| CHEMBL4856457 | — | — | 1 | 6.27 |
| CHEMBL4864747 | — | — | 1 | 6.23 |
| CHEMBL4863807 | — | — | 1 | 6.23 |
| CHEMBL4855135 | — | — | 1 | 6.22 |
| CHEMBL4848201 | — | — | 1 | 6.13 |
| CHEMBL4875870 | — | — | 1 | 6.12 |
| CHEMBL4860544 | — | — | 1 | 6.10 |
| CHEMBL4872122 | — | — | 1 | 6.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4871144 | — | Kd | = | 22.0 | nM | 7.66 |
| CHEMBL4858532 | — | Kd | = | 38.0 | nM | 7.42 |
| CHEMBL4878667 | — | Kd | = | 44.0 | nM | 7.36 |
| CHEMBL4863989 | — | Kd | = | 59.0 | nM | 7.23 |
| CHEMBL4866742 | — | Kd | = | 62.0 | nM | 7.21 |
| CHEMBL4876415 | — | Kd | = | 66.0 | nM | 7.18 |
| CHEMBL4856956 | — | Kd | = | 79.0 | nM | 7.10 |
| CHEMBL4878890 | — | Kd | = | 86.0 | nM | 7.07 |
| CHEMBL4872580 | — | Kd | = | 113.0 | nM | 6.95 |
| CHEMBL4870008 | — | Kd | = | 126.0 | nM | 6.90 |
| CHEMBL4862282 | — | Kd | = | 135.0 | nM | 6.87 |
| CHEMBL4850434 | — | Kd | = | 139.0 | nM | 6.86 |
| CHEMBL4862808 | — | Kd | = | 192.0 | nM | 6.72 |
| CHEMBL4868302 | — | Kd | = | 212.0 | nM | 6.67 |
| CHEMBL4859741 | — | Kd | = | 247.0 | nM | 6.61 |
| CHEMBL4876664 | — | Kd | = | 263.0 | nM | 6.58 |
| CHEMBL4879078 | — | Kd | = | 295.0 | nM | 6.53 |
| CHEMBL4856203 | — | Kd | = | 345.0 | nM | 6.46 |
| CHEMBL4850750 | — | Kd | = | 354.0 | nM | 6.45 |
| CHEMBL4853042 | — | Kd | = | 484.0 | nM | 6.32 |
| CHEMBL4877731 | — | Kd | = | 494.0 | nM | 6.31 |
| CHEMBL4863883 | — | Kd | = | 526.0 | nM | 6.28 |
| CHEMBL4856457 | — | Kd | = | 532.0 | nM | 6.27 |
| CHEMBL4864747 | — | Kd | = | 588.0 | nM | 6.23 |
| CHEMBL4863807 | — | Kd | = | 584.0 | nM | 6.23 |
| CHEMBL4855135 | — | Kd | = | 595.0 | nM | 6.22 |
| CHEMBL4848201 | — | Kd | = | 744.0 | nM | 6.13 |
| CHEMBL4875870 | — | Kd | = | 768.0 | nM | 6.12 |
| CHEMBL4860544 | — | Kd | = | 798.0 | nM | 6.10 |
| CHEMBL4872122 | — | Kd | = | 815.0 | nM | 6.09 |
| CHEMBL4866065 | — | Kd | = | 1006.0 | nM | 6.00 |
| CHEMBL4867024 | — | Kd | = | 1008.0 | nM | 6.00 |
| CHEMBL4874574 | — | Kd | = | 1110.0 | nM | 5.96 |
| CHEMBL4863758 | — | Kd | = | 1491.0 | nM | 5.83 |