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Assay Detail

CHEMBL3745585

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

Functional
Antiproliferative activity against HUVEC assessed as inhibition of human recombinant VEGF165-induced proliferation preincubated for 2 hrs followed by VEGF165 addition measured after 48 hrs by cell counting analysis
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HUVEC
Confidence 1 — Organism
Curated By Autocuration

Target

HUVEC (CHEMBL613979)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of anilinopyrimidine-based naphthamide derivatives as potent VEGFR-2 inhibitors
Lv Y, Li M, Cao S, Tong L, Peng T, Wei L, Xie H, Ding J, Duan W
Medchemcomm (2015) 6 : 1375 -1380
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 8.21 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3742328 1 9.70
CHEMBL3740163 1 9.10
CHEMBL3739633 1 9.10
CHEMBL3741966 1 8.92
CHEMBL491473 CEDIRANIB 3.0 1 8.92
CHEMBL3739732 1 8.80
CHEMBL3740673 1 8.80
CHEMBL3741484 1 8.72
CHEMBL3741316 1 8.70
CHEMBL3740574 1 8.66
CHEMBL3740781 1 8.62
CHEMBL3741965 1 8.60
CHEMBL3740276 1 8.48
CHEMBL3740487 1 8.48
CHEMBL3741413 1 8.38
CHEMBL3739627 1 8.24
CHEMBL3740087 1 8.17
CHEMBL3741916 1 8.11
CHEMBL3741311 1 8.09
CHEMBL3739726 1 8.04
CHEMBL3740554 1 8.03
CHEMBL3741621 1 8.03
CHEMBL3740721 1 8.01
CHEMBL3739936 1 7.97
CHEMBL3741625 1 7.86
CHEMBL3740530 1 7.83
CHEMBL3740788 1 7.72
CHEMBL3741187 1 7.71
CHEMBL3742168 1 7.59
CHEMBL3739656 1 7.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3742328 IC50 = 0.2 nM 9.70
CHEMBL3740163 IC50 = 0.8 nM 9.10
CHEMBL3739633 IC50 = 0.8 nM 9.10
CHEMBL3741966 IC50 = 1.2 nM 8.92
CHEMBL491473 CEDIRANIB IC50 = 1.2 nM 8.92
CHEMBL3739732 IC50 = 1.6 nM 8.80
CHEMBL3740673 IC50 = 1.6 nM 8.80
CHEMBL3741484 IC50 = 1.9 nM 8.72
CHEMBL3741316 IC50 = 2.0 nM 8.70
CHEMBL3740574 IC50 = 2.2 nM 8.66
CHEMBL3740781 IC50 = 2.4 nM 8.62
CHEMBL3741965 IC50 = 2.5 nM 8.60
CHEMBL3740276 IC50 = 3.3 nM 8.48
CHEMBL3740487 IC50 = 3.3 nM 8.48
CHEMBL3741413 IC50 = 4.2 nM 8.38
CHEMBL3739627 IC50 = 5.7 nM 8.24
CHEMBL3740087 IC50 = 6.8 nM 8.17
CHEMBL3741916 IC50 = 7.7 nM 8.11
CHEMBL3741311 IC50 = 8.2 nM 8.09
CHEMBL3739726 IC50 = 9.2 nM 8.04
CHEMBL3741621 IC50 = 9.3 nM 8.03
CHEMBL3740554 IC50 = 9.3 nM 8.03
CHEMBL3740721 IC50 = 9.8 nM 8.01
CHEMBL3739936 IC50 = 10.6 nM 7.97
CHEMBL3741625 IC50 = 13.7 nM 7.86
CHEMBL3740530 IC50 = 14.8 nM 7.83
CHEMBL3740788 IC50 = 19.1 nM 7.72
CHEMBL3741187 IC50 = 19.5 nM 7.71
CHEMBL3742168 IC50 = 25.6 nM 7.59
CHEMBL3739656 IC50 = 26.0 nM 7.58
CHEMBL3741592 IC50 = 26.0 nM 7.58
CHEMBL3741411 IC50 = 31.5 nM 7.50
CHEMBL3741641 IC50 = 32.2 nM 7.49
CHEMBL3739569 IC50 = 33.2 nM 7.48
CHEMBL3740856 IC50 = 41.8 nM 7.38
CHEMBL3739572 IC50 = 92.4 nM 7.03
CHEMBL3740073 IC50 > 100.0 nM -
CHEMBL3739835 IC50 > 100.0 nM -
CHEMBL3741876 IC50 > 100.0 nM -