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Assay Detail

CHEMBL5511956

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

Binding
Binding affinity to VHL (unknown origin)-NanoLuc fusion protein expressed in HEK293 cells assessed as apparent dissociation constant incubated for 2 hrs by NanoBRET assay
109
Total Activities
109
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

von Hippel-Lindau disease tumor suppressor (CHEMBL3108660)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potency-Enhanced Peptidomimetic VHL Ligands with Improved Oral Bioavailability.
Wu H, Murray J, Ishisoko N, Frommlet A, Deshmukh G, DiPasquale A, Mulvihill MM, Zhang D, Quinn JG, Blake RA, Fairbrother WJ, Fuhrmann J.
J Med Chem (2024) 67 : 8585 -8608
PubMed 38809766 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 109 5.54 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5531987 1 8.48
CHEMBL5568405 1 8.20
CHEMBL5561098 1 7.23
CHEMBL5557410 1 7.20
CHEMBL5523602 1 7.17
CHEMBL5565598 1 7.13
CHEMBL5557627 1 7.07
CHEMBL5532286 1 7.07
CHEMBL5567564 1 7.00
CHEMBL5556367 1 6.96
CHEMBL5523400 1 6.89
CHEMBL5559950 1 6.89
CHEMBL5550038 1 6.80
CHEMBL4565531 1 6.75
CHEMBL3344081 1 6.70
CHEMBL5566779 1 6.58
CHEMBL5567920 1 6.58
CHEMBL5560777 1 6.17
CHEMBL5562051 1 5.89
CHEMBL5562118 1 5.72
CHEMBL5561983 1 5.70
CHEMBL5563285 1 5.70
CHEMBL5558694 1 5.62
CHEMBL5542362 1 5.60
CHEMBL5555944 1 5.52
CHEMBL5562734 1 5.47
CHEMBL5560099 1 5.40
CHEMBL5556974 1 5.36
CHEMBL5532505 1 5.34
CHEMBL5565425 1 5.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5531987 Kd = 3.3 nM 8.48
CHEMBL5568405 Kd = 6.3 nM 8.20
CHEMBL5561098 Kd = 59.0 nM 7.23
CHEMBL5557410 Kd = 63.0 nM 7.20
CHEMBL5523602 Kd = 67.0 nM 7.17
CHEMBL5565598 Kd = 74.0 nM 7.13
CHEMBL5532286 Kd = 85.0 nM 7.07
CHEMBL5557627 Kd = 85.0 nM 7.07
CHEMBL5567564 Kd = 99.0 nM 7.00
CHEMBL5556367 Kd = 110.0 nM 6.96
CHEMBL5559950 Kd = 130.0 nM 6.89
CHEMBL5523400 Kd = 130.0 nM 6.89
CHEMBL5550038 Kd = 160.0 nM 6.80
CHEMBL4565531 Kd = 180.0 nM 6.75
CHEMBL3344081 Kd = 200.0 nM 6.70
CHEMBL5567920 Kd = 260.0 nM 6.58
CHEMBL5566779 Kd = 260.0 nM 6.58
CHEMBL5560777 Kd = 680.0 nM 6.17
CHEMBL5562051 Kd = 1300.0 nM 5.89
CHEMBL5562118 Kd = 1900.0 nM 5.72
CHEMBL5561983 Kd = 1990.0 nM 5.70
CHEMBL5563285 Kd = 2000.0 nM 5.70
CHEMBL5558694 Kd = 2400.0 nM 5.62
CHEMBL5542362 Kd = 2500.0 nM 5.60
CHEMBL5555944 Kd = 3000.0 nM 5.52
CHEMBL5562734 Kd = 3370.0 nM 5.47
CHEMBL5560099 Kd = 4000.0 nM 5.40
CHEMBL5556974 Kd = 4400.0 nM 5.36
CHEMBL5532505 Kd = 4600.0 nM 5.34
CHEMBL5565425 Kd = 5170.0 nM 5.29
CHEMBL5559916 Kd = 5500.0 nM 5.26
CHEMBL5560147 Kd = 6100.0 nM 5.21
CHEMBL5527840 Kd = 6600.0 nM 5.18
CHEMBL5517736 Kd = 6600.0 nM 5.18
CHEMBL5523429 Kd = 7000.0 nM 5.16
CHEMBL5518083 Kd = 7400.0 nM 5.13
CHEMBL5517933 Kd = 7700.0 nM 5.11
CHEMBL5556945 Kd = 7700.0 nM 5.11
CHEMBL5567365 Kd = 8700.0 nM 5.06
CHEMBL5542093 Kd = 9200.0 nM 5.04
CHEMBL5532172 Kd = 9700.0 nM 5.01
CHEMBL5560333 Kd = 10300.0 nM 4.99
CHEMBL5556018 Kd = 10500.0 nM 4.98
CHEMBL5565978 Kd = 11000.0 nM 4.96
CHEMBL5566856 Kd = 11800.0 nM 4.93
CHEMBL5562466 Kd = 12200.0 nM 4.91
CHEMBL5517989 Kd = 14000.0 nM 4.85
CHEMBL5558821 Kd = 14000.0 nM 4.85
CHEMBL5560621 Kd = 15400.0 nM 4.81
CHEMBL5560816 Kd = 17800.0 nM 4.75