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Assay Detail

CHEMBL3636058

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

Binding
Inhibition of VEGFR-2 (unknown origin) after 1 hr by ADP-Glo assay
39
Total Activities
39
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 novel VEGFR-2 inhibitors. Part 5: Exploration of diverse hinge-binding fragments via core-refining approach.
Shan Y, Gao H, Shao X, Wang J, Pan X, Zhang J.
Eur J Med Chem (2015) 103 : 80 -90
PubMed 26342134 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 7.02 9.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1336 SORAFENIB 4.0 1 9.32
CHEMBL3633294 1 9.30
CHEMBL3633304 1 9.10
CHEMBL3633684 1 8.86
CHEMBL3633292 1 8.67
CHEMBL3633296 1 8.64
CHEMBL3633295 1 8.63
CHEMBL3633686 1 8.46
CHEMBL3633298 1 7.68
CHEMBL3633271 1 7.55
CHEMBL3633303 1 7.38
CHEMBL3633290 1 7.27
CHEMBL3633291 1 7.23
CHEMBL3633273 1 7.21
CHEMBL3633293 1 6.94
CHEMBL3633302 1 6.93
CHEMBL3633277 1 6.80
CHEMBL3633301 1 6.69
CHEMBL3633297 1 6.48
CHEMBL3633288 1 5.33
CHEMBL3633275 1 5.27
CHEMBL3633280 1 5.08
CHEMBL3633289 1 4.83
CHEMBL3633278 1 4.42
CHEMBL3633276 1 4.29
CHEMBL3633274 1 4.28
CHEMBL3633281 1 -
CHEMBL3633685 1 -
CHEMBL3633305 1 -
CHEMBL3633272 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1336 SORAFENIB IC50 = 0.48 nM 9.32
CHEMBL3633294 IC50 = 0.5 nM 9.30
CHEMBL3633304 IC50 = 0.79 nM 9.10
CHEMBL3633684 IC50 = 1.38 nM 8.86
CHEMBL3633292 IC50 = 2.15 nM 8.67
CHEMBL3633296 IC50 = 2.28 nM 8.64
CHEMBL3633295 IC50 = 2.36 nM 8.63
CHEMBL3633686 IC50 = 3.47 nM 8.46
CHEMBL3633298 IC50 = 21.0 nM 7.68
CHEMBL3633271 IC50 = 28.0 nM 7.55
CHEMBL3633303 IC50 = 41.8 nM 7.38
CHEMBL3633290 IC50 = 53.6 nM 7.27
CHEMBL3633291 IC50 = 59.2 nM 7.23
CHEMBL3633273 IC50 = 62.0 nM 7.21
CHEMBL3633293 IC50 = 116.0 nM 6.94
CHEMBL3633302 IC50 = 117.0 nM 6.93
CHEMBL3633277 IC50 = 160.0 nM 6.80
CHEMBL3633301 IC50 = 205.0 nM 6.69
CHEMBL3633297 IC50 = 331.0 nM 6.48
CHEMBL3633288 IC50 = 4700.0 nM 5.33
CHEMBL3633275 IC50 = 5400.0 nM 5.27
CHEMBL3633280 IC50 = 8400.0 nM 5.08
CHEMBL3633289 IC50 = 14900.0 nM 4.83
CHEMBL3633278 IC50 = 37700.0 nM 4.42
CHEMBL3633276 IC50 = 51900.0 nM 4.29
CHEMBL3633274 IC50 = 53000.0 nM 4.28
CHEMBL3633299 IC50 > 500.0 nM -
CHEMBL3633300 IC50 > 500.0 nM -
CHEMBL3633287 IC50 > 500000.0 nM -
CHEMBL3633286 IC50 > 500000.0 nM -
CHEMBL3633285 IC50 > 500000.0 nM -
CHEMBL3633284 IC50 > 500000.0 nM -
CHEMBL3633283 IC50 > 500000.0 nM -
CHEMBL3633282 IC50 > 500000.0 nM -
CHEMBL3633279 IC50 > 500000.0 nM -
CHEMBL3633272 IC50 > 500000.0 nM -
CHEMBL3633305 IC50 > 500.0 nM -
CHEMBL3633685 IC50 > 500.0 nM -
CHEMBL3633281 IC50 > 500000.0 nM -