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Assay Detail

CHEMBL3399480

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

Binding
Inhibition of VEGFR2 (unknown origin) using ATP measured luminescence by ADP-Glo Kinase assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Vascular endothelial growth factor receptor 2 (CHEMBL279)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of biphenyl-based VEGFR-2 inhibitors. Part 3: design, synthesis and 3D-QSAR studies.
Lu W, Li P, Shan Y, Su P, Wang J, Shi Y, Zhang J.
Bioorg Med Chem (2015) 23 : 1044 -1054
PubMed 25637123 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 7.38 9.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1336 SORAFENIB 4.0 1 9.07
CHEMBL3397933 1 8.70
CHEMBL3397917 1 8.36
CHEMBL3397935 1 8.31
CHEMBL3397934 1 8.06
CHEMBL3397920 1 8.03
CHEMBL3397932 1 7.84
CHEMBL3397918 1 7.82
CHEMBL3397942 1 7.75
CHEMBL3397923 1 7.64
CHEMBL3397940 1 7.56
CHEMBL3397928 1 7.50
CHEMBL3397936 1 7.35
CHEMBL3397931 1 7.27
CHEMBL3397930 1 7.20
CHEMBL3397915 1 7.16
CHEMBL3397946 1 7.14
CHEMBL3397944 1 7.11
CHEMBL3397939 1 7.07
CHEMBL3397924 1 7.02
CHEMBL3397945 1 6.90
CHEMBL3397937 1 6.89
CHEMBL3397922 1 6.88
CHEMBL3397941 1 6.80
CHEMBL3397916 1 6.74
CHEMBL3397929 1 6.67
CHEMBL3397947 1 6.46
CHEMBL3397927 1 6.44
CHEMBL3397925 1 6.20
CHEMBL3397943 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1336 SORAFENIB IC50 = 0.85 nM 9.07
CHEMBL3397933 IC50 = 2.02 nM 8.70
CHEMBL3397917 IC50 = 4.38 nM 8.36
CHEMBL3397935 IC50 = 4.86 nM 8.31
CHEMBL3397934 IC50 = 8.74 nM 8.06
CHEMBL3397920 IC50 = 9.41 nM 8.03
CHEMBL3397932 IC50 = 14.48 nM 7.84
CHEMBL3397918 IC50 = 15.04 nM 7.82
CHEMBL3397942 IC50 = 17.85 nM 7.75
CHEMBL3397923 IC50 = 22.85 nM 7.64
CHEMBL3397940 IC50 = 27.58 nM 7.56
CHEMBL3397928 IC50 = 31.98 nM 7.50
CHEMBL3397936 IC50 = 44.32 nM 7.35
CHEMBL3397931 IC50 = 54.26 nM 7.27
CHEMBL3397930 IC50 = 62.52 nM 7.20
CHEMBL3397915 IC50 = 69.4 nM 7.16
CHEMBL3397946 IC50 = 71.89 nM 7.14
CHEMBL3397944 IC50 = 77.45 nM 7.11
CHEMBL3397939 IC50 = 85.32 nM 7.07
CHEMBL3397924 IC50 = 94.69 nM 7.02
CHEMBL3397945 IC50 = 125.82 nM 6.90
CHEMBL3397937 IC50 = 129.25 nM 6.89
CHEMBL3397922 IC50 = 130.17 nM 6.88
CHEMBL3397941 IC50 = 158.46 nM 6.80
CHEMBL3397916 IC50 = 182.82 nM 6.74
CHEMBL3397929 IC50 = 214.87 nM 6.67
CHEMBL3397947 IC50 = 344.61 nM 6.46
CHEMBL3397927 IC50 = 359.63 nM 6.44
CHEMBL3397925 IC50 = 624.66 nM 6.20
CHEMBL3397943 IC50 - -
CHEMBL3397938 IC50 - -
CHEMBL3397919 IC50 - -
CHEMBL3397921 IC50 - -
CHEMBL3397926 IC50 - -