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Assay Detail

CHEMBL1763555

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

Binding
Inhibition of recombinant human VEGFR-2-mediated poly(Glu4Tyr) phosphorylation after 1 hr
38
Total Activities
38
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

Impact of aryloxy-linked quinazolines: a novel series of selective VEGFR-2 receptor tyrosine kinase inhibitors.
Garofalo A, Goossens L, Six P, Lemoine A, Ravez S, Farce A, Depreux P.
Bioorg Med Chem Lett (2011) 21 : 2106 -2112
PubMed 21353546 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 6.15 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1761942 1 7.52
CHEMBL1761939 1 7.40
CHEMBL1761937 1 7.30
CHEMBL1761941 1 7.30
CHEMBL1277162 1 7.22
CHEMBL1761940 1 7.22
CHEMBL179603 1 7.16
CHEMBL1761938 1 7.05
CHEMBL24828 VANDETANIB 4.0 1 7.00
CHEMBL1761936 1 6.40
CHEMBL1761932 1 6.22
CHEMBL1278149 1 6.22
CHEMBL1277254 1 6.22
CHEMBL1277253 1 6.22
CHEMBL1761930 1 6.16
CHEMBL205089 1 6.00
CHEMBL1277620 1 5.78
CHEMBL1761944 1 5.37
CHEMBL1761933 1 5.29
CHEMBL301018 1 5.28
CHEMBL1761943 1 5.26
CHEMBL1761931 1 5.25
CHEMBL1761929 1 5.24
CHEMBL1761934 1 5.21
CHEMBL1278148 1 5.02
CHEMBL98798 1 5.01
CHEMBL939 GEFITINIB 4.0 1 4.83
CHEMBL1276893 1 -
CHEMBL1276892 1 -
CHEMBL1761935 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1761942 IC50 = 30.0 nM 7.52
CHEMBL1761939 IC50 = 40.0 nM 7.40
CHEMBL1761941 IC50 = 50.0 nM 7.30
CHEMBL1761937 IC50 = 50.0 nM 7.30
CHEMBL1277162 IC50 = 60.0 nM 7.22
CHEMBL1761940 IC50 = 60.0 nM 7.22
CHEMBL179603 IC50 = 70.0 nM 7.16
CHEMBL1761938 IC50 = 90.0 nM 7.05
CHEMBL24828 VANDETANIB IC50 = 100.0 nM 7.00
CHEMBL1761936 IC50 = 400.0 nM 6.40
CHEMBL1278149 IC50 = 600.0 nM 6.22
CHEMBL1277253 IC50 = 600.0 nM 6.22
CHEMBL1277254 IC50 = 600.0 nM 6.22
CHEMBL1761932 IC50 = 600.0 nM 6.22
CHEMBL1761930 IC50 = 700.0 nM 6.16
CHEMBL205089 IC50 = 1000.0 nM 6.00
CHEMBL1277620 IC50 = 1650.0 nM 5.78
CHEMBL1761944 IC50 = 4300.0 nM 5.37
CHEMBL1761933 IC50 = 5100.0 nM 5.29
CHEMBL301018 IC50 = 5300.0 nM 5.28
CHEMBL1761943 IC50 = 5500.0 nM 5.26
CHEMBL1761931 IC50 = 5600.0 nM 5.25
CHEMBL1761929 IC50 = 5800.0 nM 5.24
CHEMBL1761934 IC50 = 6200.0 nM 5.21
CHEMBL1278148 IC50 = 9500.0 nM 5.02
CHEMBL98798 IC50 = 9800.0 nM 5.01
CHEMBL939 GEFITINIB IC50 = 14800.0 nM 4.83
CHEMBL29197 IC50 - -
CHEMBL1761945 IC50 > 10000.0 nM -
CHEMBL447230 IC50 > 10000.0 nM -
CHEMBL1278056 IC50 > 10000.0 nM -
CHEMBL1278057 IC50 > 10000.0 nM -
CHEMBL1761927 IC50 > 10000.0 nM -
CHEMBL1761928 IC50 > 10000.0 nM -
CHEMBL1278235 IC50 > 10000.0 nM -
CHEMBL1761935 IC50 > 10000.0 nM -
CHEMBL1276892 IC50 > 10000.0 nM -
CHEMBL1276893 IC50 > 10000.0 nM -