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Assay Detail

CHEMBL5735545

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Fluorescence Polarization Assay (10% 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 (10% DMSO).
ChEMBL ↗
261
Total Activities
87
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
(2020)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 87 5.63 7.79
kon 87 - -
k_off 87 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5757017 — — 3 7.79
CHEMBL5950547 — — 3 6.58
CHEMBL5865930 — — 3 6.53
CHEMBL6022352 — — 3 6.50
CHEMBL5916082 — — 3 6.47
CHEMBL5815328 — — 3 6.46
CHEMBL6010538 — — 3 6.36
CHEMBL5753441 — — 3 6.33
CHEMBL6031446 — — 3 6.30
CHEMBL5814107 — — 3 6.27
CHEMBL5814612 — — 3 6.24
CHEMBL5872191 — — 3 6.17
CHEMBL5859828 — — 3 6.09
CHEMBL5843680 — — 3 6.07
CHEMBL5947789 — — 3 5.99
CHEMBL5776955 — — 3 5.99
CHEMBL5877102 — — 3 5.97
CHEMBL5816245 — — 3 5.97
CHEMBL6004202 — — 3 5.96
CHEMBL5808824 — — 3 5.94
CHEMBL5861665 — — 3 5.93
CHEMBL5936928 — — 3 5.92
CHEMBL5940890 — — 3 5.92
CHEMBL5988952 — — 3 5.92
CHEMBL5974485 — — 3 5.92
CHEMBL5897863 — — 3 5.89
CHEMBL6031191 — — 3 5.88
CHEMBL5806530 — — 3 5.86
CHEMBL6020386 — — 3 5.85
CHEMBL5964291 — — 3 5.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5757017 — IC50 = 16.3 nM 7.79
CHEMBL5950547 — IC50 = 264.0 nM 6.58
CHEMBL5865930 — IC50 = 293.0 nM 6.53
CHEMBL6022352 — IC50 = 320.0 nM 6.50
CHEMBL5916082 — IC50 = 339.0 nM 6.47
CHEMBL5815328 — IC50 = 349.0 nM 6.46
CHEMBL6010538 — IC50 = 441.0 nM 6.36
CHEMBL5753441 — IC50 = 465.0 nM 6.33
CHEMBL6031446 — IC50 = 498.0 nM 6.30
CHEMBL5814107 — IC50 = 533.0 nM 6.27
CHEMBL5814612 — IC50 = 578.0 nM 6.24
CHEMBL5872191 — IC50 = 668.0 nM 6.17
CHEMBL5859828 — IC50 = 810.0 nM 6.09
CHEMBL5843680 — IC50 = 859.0 nM 6.07
CHEMBL5776955 — IC50 = 1030.0 nM 5.99
CHEMBL5947789 — IC50 = 1030.0 nM 5.99
CHEMBL5877102 — IC50 = 1080.0 nM 5.97
CHEMBL5816245 — IC50 = 1070.0 nM 5.97
CHEMBL6004202 — IC50 = 1090.0 nM 5.96
CHEMBL5808824 — IC50 = 1150.0 nM 5.94
CHEMBL5861665 — IC50 = 1180.0 nM 5.93
CHEMBL5936928 — IC50 = 1200.0 nM 5.92
CHEMBL5940890 — IC50 = 1200.0 nM 5.92
CHEMBL5974485 — IC50 = 1210.0 nM 5.92
CHEMBL5988952 — IC50 = 1190.0 nM 5.92
CHEMBL5897863 — IC50 = 1300.0 nM 5.89
CHEMBL6031191 — IC50 = 1330.0 nM 5.88
CHEMBL5806530 — IC50 = 1380.0 nM 5.86
CHEMBL6020386 — IC50 = 1410.0 nM 5.85
CHEMBL5964291 — IC50 = 1460.0 nM 5.84
CHEMBL3344081 — IC50 = 1480.0 nM 5.83
CHEMBL4783485 — IC50 = 1490.0 nM 5.83
CHEMBL5830270 — IC50 = 1480.0 nM 5.83
CHEMBL5913553 — IC50 = 1480.0 nM 5.83
CHEMBL6028774 — IC50 = 1580.0 nM 5.80
CHEMBL5949083 — IC50 = 1580.0 nM 5.80
CHEMBL5743803 — IC50 = 1630.0 nM 5.79
CHEMBL6009432 — IC50 = 1670.0 nM 5.78
CHEMBL5906897 — IC50 = 1650.0 nM 5.78
CHEMBL6055637 — IC50 = 1800.0 nM 5.75
CHEMBL5821522 — IC50 = 1850.0 nM 5.73
CHEMBL5752262 — IC50 = 1940.0 nM 5.71
CHEMBL5784353 — IC50 = 2110.0 nM 5.68
CHEMBL5868625 — IC50 = 2280.0 nM 5.64
CHEMBL6020910 — IC50 = 2720.0 nM 5.57
CHEMBL5936060 — IC50 = 2940.0 nM 5.53
CHEMBL5841548 — IC50 = 3050.0 nM 5.52
CHEMBL5835454 — IC50 = 3360.0 nM 5.47
CHEMBL6032589 — IC50 = 3600.0 nM 5.44
CHEMBL5850407 — IC50 = 3730.0 nM 5.43