Assay Detail
Binding
CHEMBL5735546
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Fluorescence Polarization Assay (0.25% 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 (0.25% DMSO).
111
Total Activities
37
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 | 37 | 5.52 | 6.02 |
| kon | 37 | - | - |
| k_off | 37 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5743803 | — | — | 3 | 6.02 |
| CHEMBL5741022 | — | — | 3 | 5.94 |
| CHEMBL5850058 | — | — | 3 | 5.91 |
| CHEMBL6031446 | — | — | 3 | 5.89 |
| CHEMBL6047184 | — | — | 3 | 5.86 |
| CHEMBL5757017 | — | — | 3 | 5.81 |
| CHEMBL5790714 | — | — | 3 | 5.80 |
| CHEMBL5802355 | — | — | 3 | 5.72 |
| CHEMBL5877102 | — | — | 3 | 5.71 |
| CHEMBL5897863 | — | — | 3 | 5.69 |
| CHEMBL5861665 | — | — | 3 | 5.67 |
| CHEMBL6004202 | — | — | 3 | 5.66 |
| CHEMBL5816245 | — | — | 3 | 5.66 |
| CHEMBL5835454 | — | — | 3 | 5.65 |
| CHEMBL5843680 | — | — | 3 | 5.64 |
| CHEMBL5821522 | — | — | 3 | 5.62 |
| CHEMBL6009432 | — | — | 3 | 5.62 |
| CHEMBL3344081 | — | — | 3 | 5.59 |
| CHEMBL5814107 | — | — | 3 | 5.54 |
| CHEMBL6010538 | — | — | 3 | 5.53 |
| CHEMBL6055637 | — | — | 3 | 5.53 |
| CHEMBL6031191 | — | — | 3 | 5.52 |
| CHEMBL5784353 | — | — | 3 | 5.49 |
| CHEMBL5752262 | — | — | 3 | 5.48 |
| CHEMBL5936060 | — | — | 3 | 5.47 |
| CHEMBL5906897 | — | — | 3 | 5.42 |
| CHEMBL6032589 | — | — | 3 | 5.35 |
| CHEMBL5808824 | — | — | 3 | 5.30 |
| CHEMBL6020910 | — | — | 3 | 5.26 |
| CHEMBL4783485 | — | — | 3 | 5.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5743803 | — | IC50 | = | 958.0 | nM | 6.02 |
| CHEMBL5741022 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL5850058 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL6031446 | — | IC50 | = | 1280.0 | nM | 5.89 |
| CHEMBL6047184 | — | IC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL5757017 | — | IC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL5790714 | — | IC50 | = | 1569.0 | nM | 5.80 |
| CHEMBL5802355 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL5877102 | — | IC50 | = | 1940.0 | nM | 5.71 |
| CHEMBL5897863 | — | IC50 | = | 2050.0 | nM | 5.69 |
| CHEMBL5861665 | — | IC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL6004202 | — | IC50 | = | 2190.0 | nM | 5.66 |
| CHEMBL5816245 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL5835454 | — | IC50 | = | 2220.0 | nM | 5.65 |
| CHEMBL5843680 | — | IC50 | = | 2270.0 | nM | 5.64 |
| CHEMBL6009432 | — | IC50 | = | 2380.0 | nM | 5.62 |
| CHEMBL5821522 | — | IC50 | = | 2420.0 | nM | 5.62 |
| CHEMBL3344081 | — | IC50 | = | 2540.0 | nM | 5.59 |
| CHEMBL5814107 | — | IC50 | = | 2860.0 | nM | 5.54 |
| CHEMBL6010538 | — | IC50 | = | 2940.0 | nM | 5.53 |
| CHEMBL6055637 | — | IC50 | = | 2950.0 | nM | 5.53 |
| CHEMBL6031191 | — | IC50 | = | 3040.0 | nM | 5.52 |
| CHEMBL5784353 | — | IC50 | = | 3220.0 | nM | 5.49 |
| CHEMBL5752262 | — | IC50 | = | 3340.0 | nM | 5.48 |
| CHEMBL5936060 | — | IC50 | = | 3370.0 | nM | 5.47 |
| CHEMBL5906897 | — | IC50 | = | 3770.0 | nM | 5.42 |
| CHEMBL6032589 | — | IC50 | = | 4470.0 | nM | 5.35 |
| CHEMBL5808824 | — | IC50 | = | 4960.0 | nM | 5.30 |
| CHEMBL6020910 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL4783485 | — | IC50 | = | 5690.0 | nM | 5.25 |
| CHEMBL5913553 | — | IC50 | = | 6370.0 | nM | 5.20 |
| CHEMBL5866480 | — | IC50 | = | 6540.0 | nM | 5.18 |
| CHEMBL5874684 | — | IC50 | = | 7150.0 | nM | 5.15 |
| CHEMBL5841548 | — | IC50 | = | 7280.0 | nM | 5.14 |
| CHEMBL5949083 | — | IC50 | = | 7720.0 | nM | 5.11 |
| CHEMBL4228328 | — | IC50 | = | 9340.0 | nM | 5.03 |
| CHEMBL5929983 | — | IC50 | = | 17500.0 | nM | 4.76 |
| CHEMBL5802355 | — | k_off | = | - | s-1 | - |
| CHEMBL5866480 | — | k_off | = | - | s-1 | - |
| CHEMBL5843680 | — | k_off | = | - | s-1 | - |
| CHEMBL5843680 | — | kon | = | - | — | - |
| CHEMBL5841548 | — | kon | = | - | — | - |
| CHEMBL5821522 | — | k_off | = | - | s-1 | - |
| CHEMBL5841548 | — | k_off | = | - | s-1 | - |
| CHEMBL5821522 | — | kon | = | - | — | - |
| CHEMBL6032589 | — | k_off | = | - | s-1 | - |
| CHEMBL6032589 | — | kon | = | - | — | - |
| CHEMBL5790714 | — | k_off | = | - | s-1 | - |
| CHEMBL5929983 | — | kon | = | - | — | - |
| CHEMBL5741022 | — | kon | = | - | — | - |