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Assay Detail

CHEMBL5368610

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

Binding
Binding affinity to N-terminal His6-tagged VHL (54 to 213 residues)/Elongin B/Elogin C (unknown origin) using (FAM)-labeled HIF-1alpha peptide as substrate assessed as dissociation constant by fluorescence polarization assay
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Publication

Expanding the Structural Diversity at the Phenylene Core of Ligands for the von Hippel-Lindau E3 Ubiquitin Ligase: Development of Highly Potent Hypoxia-Inducible Factor-1α Stabilizers.
Vu LP, Diehl CJ, Casement R, Bond AG, Steinebach C, Strašek N, Bricelj A, Perdih A, Schnakenburg G, Sosič I, Ciulli A, Gütschow M.
J Med Chem (2023) 66 : 12776 -12811
PubMed 37708384 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 37 6.43 7.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5421220 1 7.43
CHEMBL5403921 1 7.28
CHEMBL5425778 1 7.20
CHEMBL5398197 1 7.14
CHEMBL5422221 1 7.10
CHEMBL5416084 1 7.07
CHEMBL5423283 1 7.01
CHEMBL5405990 1 6.95
CHEMBL4225537 1 6.89
CHEMBL5425050 1 6.87
CHEMBL5424186 1 6.85
CHEMBL5413837 1 6.83
CHEMBL5395747 1 6.79
CHEMBL5412800 1 6.79
CHEMBL5416976 1 6.74
CHEMBL5430466 1 6.73
CHEMBL5412363 1 6.66
CHEMBL5414027 1 6.61
CHEMBL5418347 1 6.55
CHEMBL5422644 1 6.53
CHEMBL5405666 1 6.52
CHEMBL5401657 1 6.49
CHEMBL5435739 1 6.48
CHEMBL5423266 1 6.40
CHEMBL5404633 1 6.30
CHEMBL5397830 1 6.28
CHEMBL5398219 1 6.05
CHEMBL5420043 1 5.98
CHEMBL5402376 1 5.90
CHEMBL5410571 1 5.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5421220 Kd = 37.0 nM 7.43
CHEMBL5403921 Kd = 53.0 nM 7.28
CHEMBL5425778 Kd = 63.0 nM 7.20
CHEMBL5398197 Kd = 73.0 nM 7.14
CHEMBL5422221 Kd = 80.0 nM 7.10
CHEMBL5416084 Kd = 86.0 nM 7.07
CHEMBL5423283 Kd = 97.0 nM 7.01
CHEMBL5405990 Kd = 112.0 nM 6.95
CHEMBL4225537 Kd = 129.0 nM 6.89
CHEMBL5425050 Kd = 134.0 nM 6.87
CHEMBL5424186 Kd = 141.0 nM 6.85
CHEMBL5413837 Kd = 149.0 nM 6.83
CHEMBL5395747 Kd = 163.0 nM 6.79
CHEMBL5412800 Kd = 162.0 nM 6.79
CHEMBL5416976 Kd = 183.0 nM 6.74
CHEMBL5430466 Kd = 186.0 nM 6.73
CHEMBL5412363 Kd = 220.0 nM 6.66
CHEMBL5414027 Kd = 245.0 nM 6.61
CHEMBL5418347 Kd = 281.0 nM 6.55
CHEMBL5422644 Kd = 297.0 nM 6.53
CHEMBL5405666 Kd = 305.0 nM 6.52
CHEMBL5401657 Kd = 322.0 nM 6.49
CHEMBL5435739 Kd = 330.0 nM 6.48
CHEMBL5423266 Kd = 397.0 nM 6.40
CHEMBL5404633 Kd = 496.0 nM 6.30
CHEMBL5397830 Kd = 528.0 nM 6.28
CHEMBL5398219 Kd = 883.0 nM 6.05
CHEMBL5420043 Kd = 1040.0 nM 5.98
CHEMBL5402376 Kd = 1270.0 nM 5.90
CHEMBL5410571 Kd = 1450.0 nM 5.84
CHEMBL5436460 Kd = 2130.0 nM 5.67
CHEMBL5433809 Kd = 2550.0 nM 5.59
CHEMBL5395402 Kd = 3920.0 nM 5.41
CHEMBL5432818 Kd = 4040.0 nM 5.39
CHEMBL5408755 Kd = 4110.0 nM 5.39
CHEMBL5426675 Kd = 6240.0 nM 5.21
CHEMBL5406835 Kd = 8150.0 nM 5.09