Assay Detail
Binding
CHEMBL4835128
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 FKBP12.6 (unknown origin) expressed in Escherichia coli BL21 (DE3) cells incubated for 30 mins by fluorescence polarisation competition 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 FKBP1B (CHEMBL2430) ↗| 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 | 6.78 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4871144 | — | — | 1 | 8.05 |
| CHEMBL4878667 | — | — | 1 | 7.72 |
| CHEMBL4858532 | — | — | 1 | 7.70 |
| CHEMBL4863989 | — | — | 1 | 7.50 |
| CHEMBL4878890 | — | — | 1 | 7.42 |
| CHEMBL4876415 | — | — | 1 | 7.37 |
| CHEMBL4866742 | — | — | 1 | 7.28 |
| CHEMBL4872580 | — | — | 1 | 7.21 |
| CHEMBL4859741 | — | — | 1 | 7.09 |
| CHEMBL4856956 | — | — | 1 | 7.07 |
| CHEMBL4879078 | — | — | 1 | 7.03 |
| CHEMBL4870008 | — | — | 1 | 7.00 |
| CHEMBL4862808 | — | — | 1 | 6.98 |
| CHEMBL4850434 | — | — | 1 | 6.94 |
| CHEMBL4862282 | — | — | 1 | 6.94 |
| CHEMBL4876664 | — | — | 1 | 6.69 |
| CHEMBL4868302 | — | — | 1 | 6.67 |
| CHEMBL4850750 | — | — | 1 | 6.64 |
| CHEMBL4856457 | — | — | 1 | 6.64 |
| CHEMBL4853042 | — | — | 1 | 6.56 |
| CHEMBL4856203 | — | — | 1 | 6.52 |
| CHEMBL4855135 | — | — | 1 | 6.47 |
| CHEMBL4860544 | — | — | 1 | 6.46 |
| CHEMBL4877731 | — | — | 1 | 6.45 |
| CHEMBL4863807 | — | — | 1 | 6.42 |
| CHEMBL4874574 | — | — | 1 | 6.37 |
| CHEMBL4848201 | — | — | 1 | 6.35 |
| CHEMBL4863883 | — | — | 1 | 6.30 |
| CHEMBL4875870 | — | — | 1 | 6.22 |
| CHEMBL4872122 | — | — | 1 | 6.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4871144 | — | Kd | = | 9.0 | nM | 8.05 |
| CHEMBL4878667 | — | Kd | = | 19.0 | nM | 7.72 |
| CHEMBL4858532 | — | Kd | = | 20.0 | nM | 7.70 |
| CHEMBL4863989 | — | Kd | = | 32.0 | nM | 7.50 |
| CHEMBL4878890 | — | Kd | = | 38.0 | nM | 7.42 |
| CHEMBL4876415 | — | Kd | = | 43.0 | nM | 7.37 |
| CHEMBL4866742 | — | Kd | = | 53.0 | nM | 7.28 |
| CHEMBL4872580 | — | Kd | = | 62.0 | nM | 7.21 |
| CHEMBL4859741 | — | Kd | = | 82.0 | nM | 7.09 |
| CHEMBL4856956 | — | Kd | = | 85.0 | nM | 7.07 |
| CHEMBL4879078 | — | Kd | = | 94.0 | nM | 7.03 |
| CHEMBL4870008 | — | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL4862808 | — | Kd | = | 105.0 | nM | 6.98 |
| CHEMBL4850434 | — | Kd | = | 116.0 | nM | 6.94 |
| CHEMBL4862282 | — | Kd | = | 115.0 | nM | 6.94 |
| CHEMBL4876664 | — | Kd | = | 203.0 | nM | 6.69 |
| CHEMBL4868302 | — | Kd | = | 216.0 | nM | 6.67 |
| CHEMBL4850750 | — | Kd | = | 227.0 | nM | 6.64 |
| CHEMBL4856457 | — | Kd | = | 227.0 | nM | 6.64 |
| CHEMBL4853042 | — | Kd | = | 277.0 | nM | 6.56 |
| CHEMBL4856203 | — | Kd | = | 301.0 | nM | 6.52 |
| CHEMBL4855135 | — | Kd | = | 335.0 | nM | 6.47 |
| CHEMBL4860544 | — | Kd | = | 344.0 | nM | 6.46 |
| CHEMBL4877731 | — | Kd | = | 352.0 | nM | 6.45 |
| CHEMBL4863807 | — | Kd | = | 383.0 | nM | 6.42 |
| CHEMBL4874574 | — | Kd | = | 429.0 | nM | 6.37 |
| CHEMBL4848201 | — | Kd | = | 446.0 | nM | 6.35 |
| CHEMBL4863883 | — | Kd | = | 495.0 | nM | 6.30 |
| CHEMBL4875870 | — | Kd | = | 606.0 | nM | 6.22 |
| CHEMBL4872122 | — | Kd | = | 658.0 | nM | 6.18 |
| CHEMBL4866065 | — | Kd | = | 715.0 | nM | 6.15 |
| CHEMBL4864747 | — | Kd | = | 709.0 | nM | 6.15 |
| CHEMBL4863758 | — | Kd | = | 849.0 | nM | 6.07 |
| CHEMBL4867024 | — | Kd | = | 1075.0 | nM | 5.97 |