Assay Detail
Binding
CHEMBL5735544
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Fluorescence Polarization Assay (1% DMSO): Ability of VHL ligands to compete for the HIF 1 a binding site on VCB was determined through a fluorescence polarization competition assay as described in Buckley et al. JACS, 2012, 134, 4465-4468, WO 2013/106643, and US 2014-0356322, which are incorporated herein by reference in their entirety for all purposes (1% DMSO).
414
Total Activities
134
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
von Hippel-Lindau disease tumor suppressor (CHEMBL3108660) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Compounds and methods for the enhanced degradation of targeted proteins
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 138 | 5.55 | 7.15 |
| kon | 138 | - | - |
| k_off | 138 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5910207 | — | — | 3 | 7.15 |
| CHEMBL5556117 | — | — | 6 | 7.00 |
| CHEMBL5958158 | — | — | 3 | 6.77 |
| CHEMBL5916082 | — | — | 3 | 6.75 |
| CHEMBL6055637 | — | — | 3 | 6.58 |
| CHEMBL6031446 | — | — | 3 | 6.51 |
| CHEMBL5816245 | — | — | 3 | 6.50 |
| CHEMBL5753441 | — | — | 3 | 6.42 |
| CHEMBL4783485 | — | — | 3 | 6.41 |
| CHEMBL5997515 | — | — | 3 | 6.38 |
| CHEMBL5950547 | — | — | 3 | 6.35 |
| CHEMBL5776955 | — | — | 3 | 6.32 |
| CHEMBL5897863 | — | — | 3 | 6.29 |
| CHEMBL5757017 | — | — | 3 | 6.27 |
| CHEMBL5877102 | — | — | 3 | 6.27 |
| CHEMBL5815328 | — | — | 3 | 6.26 |
| CHEMBL5864197 | — | — | 3 | 6.25 |
| CHEMBL5843680 | — | — | 3 | 6.24 |
| CHEMBL6031191 | — | — | 3 | 6.21 |
| CHEMBL5814612 | — | — | 3 | 6.20 |
| CHEMBL6022352 | — | — | 3 | 6.20 |
| CHEMBL5861665 | — | — | 3 | 6.18 |
| CHEMBL3344081 | — | — | 3 | 6.16 |
| CHEMBL5913553 | — | — | 6 | 6.16 |
| CHEMBL5743803 | — | — | 3 | 6.16 |
| CHEMBL6020386 | — | — | 3 | 6.14 |
| CHEMBL5814107 | — | — | 3 | 6.13 |
| CHEMBL6004202 | — | — | 3 | 6.12 |
| CHEMBL5949083 | — | — | 3 | 6.10 |
| CHEMBL5974485 | — | — | 3 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5910207 | — | IC50 | = | 70.9 | nM | 7.15 |
| CHEMBL5556117 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5958158 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL5916082 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL6055637 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL6031446 | — | IC50 | = | 309.0 | nM | 6.51 |
| CHEMBL5816245 | — | IC50 | = | 317.0 | nM | 6.50 |
| CHEMBL5753441 | — | IC50 | = | 385.0 | nM | 6.42 |
| CHEMBL4783485 | — | IC50 | = | 392.0 | nM | 6.41 |
| CHEMBL5997515 | — | IC50 | = | 418.0 | nM | 6.38 |
| CHEMBL5950547 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL5776955 | — | IC50 | = | 474.0 | nM | 6.32 |
| CHEMBL5897863 | — | IC50 | = | 509.0 | nM | 6.29 |
| CHEMBL5757017 | — | IC50 | = | 542.0 | nM | 6.27 |
| CHEMBL5877102 | — | IC50 | = | 539.0 | nM | 6.27 |
| CHEMBL5815328 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5864197 | — | IC50 | = | 566.0 | nM | 6.25 |
| CHEMBL5843680 | — | IC50 | = | 572.0 | nM | 6.24 |
| CHEMBL6031191 | — | IC50 | = | 619.0 | nM | 6.21 |
| CHEMBL5814612 | — | IC50 | = | 631.0 | nM | 6.20 |
| CHEMBL6022352 | — | IC50 | = | 626.0 | nM | 6.20 |
| CHEMBL5861665 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL3344081 | — | IC50 | = | 696.0 | nM | 6.16 |
| CHEMBL5913553 | — | IC50 | = | 697.0 | nM | 6.16 |
| CHEMBL5743803 | — | IC50 | = | 699.0 | nM | 6.16 |
| CHEMBL6020386 | — | IC50 | = | 717.0 | nM | 6.14 |
| CHEMBL5814107 | — | IC50 | = | 732.0 | nM | 6.13 |
| CHEMBL6004202 | — | IC50 | = | 758.0 | nM | 6.12 |
| CHEMBL5949083 | — | IC50 | = | 799.0 | nM | 6.10 |
| CHEMBL5974485 | — | IC50 | = | 834.0 | nM | 6.08 |
| CHEMBL6020910 | — | IC50 | = | 855.0 | nM | 6.07 |
| CHEMBL6005756 | — | IC50 | = | 859.0 | nM | 6.07 |
| CHEMBL5947789 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL5830270 | — | IC50 | = | 878.0 | nM | 6.06 |
| CHEMBL5821522 | — | IC50 | = | 905.0 | nM | 6.04 |
| CHEMBL5940890 | — | IC50 | = | 906.0 | nM | 6.04 |
| CHEMBL5906897 | — | IC50 | = | 937.0 | nM | 6.03 |
| CHEMBL6010538 | — | IC50 | = | 941.0 | nM | 6.03 |
| CHEMBL5950712 | — | IC50 | = | 964.0 | nM | 6.02 |
| CHEMBL5872191 | — | IC50 | = | 972.0 | nM | 6.01 |
| CHEMBL5859828 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL5808824 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL5982814 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL5835454 | — | IC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL5841548 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL5740193 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL5752262 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL5964291 | — | IC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL5784353 | — | IC50 | = | 1280.0 | nM | 5.89 |
| CHEMBL6009432 | — | IC50 | = | 1330.0 | nM | 5.88 |