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Assay Detail

CHEMBL5553573

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

Binding
Inhibition of human recombinant VEGFR2 (805 to 1356 residues) in presence of ATP by ELISA analysis
19
Total Activities
19
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 new 1,3-diphenylurea appended aryl pyridine derivatives as apoptosis inducers through c-MET and VEGFR-2 inhibition: design, synthesis, <i>in vivo</i> and <i>in silico</i> studies.
Elsebaie HA, Nafie MS, Tawfik HO, Belal A, Ghoneim MM, Obaidullah AJ, Shaaban S, Ayed AA, El-Naggar M, Mehany ABM, Shaldam MA.
RSC Med Chem (2024) 15 : 2553 -2569
PubMed 39026631 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.70 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1289601 LENVATINIB 4.0 1 8.40
CHEMBL1946170 REGORAFENIB 4.0 1 8.38
CHEMBL5594061 1 7.62
CHEMBL2105717 CABOZANTINIB 4.0 1 7.60
CHEMBL3764045 TAS-115 1.0 1 7.52
CHEMBL5593609 1 7.46
CHEMBL1336 SORAFENIB 4.0 1 7.05
CHEMBL5571331 1 6.54
CHEMBL5574745 1 6.51
CHEMBL5568824 1 6.50
CHEMBL5595346 1 6.12
CHEMBL5575208 1 6.07
CHEMBL5565651 1 6.07
CHEMBL5583996 1 6.04
CHEMBL5574737 1 5.96
CHEMBL5565430 1 5.93
CHEMBL5572702 1 5.85
CHEMBL5579755 1 5.80
CHEMBL5574727 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1289601 LENVATINIB IC50 = 4.0 nM 8.40
CHEMBL1946170 REGORAFENIB IC50 = 4.2 nM 8.38
CHEMBL5594061 IC50 = 24.0 nM 7.62
CHEMBL2105717 CABOZANTINIB IC50 = 25.0 nM 7.60
CHEMBL3764045 TAS-115 IC50 = 30.0 nM 7.52
CHEMBL5593609 IC50 = 35.0 nM 7.46
CHEMBL1336 SORAFENIB IC50 = 90.0 nM 7.05
CHEMBL5571331 IC50 = 290.0 nM 6.54
CHEMBL5574745 IC50 = 310.0 nM 6.51
CHEMBL5568824 IC50 = 320.0 nM 6.50
CHEMBL5595346 IC50 = 750.0 nM 6.12
CHEMBL5575208 IC50 = 850.0 nM 6.07
CHEMBL5565651 IC50 = 860.0 nM 6.07
CHEMBL5583996 IC50 = 920.0 nM 6.04
CHEMBL5574737 IC50 = 1100.0 nM 5.96
CHEMBL5565430 IC50 = 1170.0 nM 5.93
CHEMBL5572702 IC50 = 1420.0 nM 5.85
CHEMBL5579755 IC50 = 1580.0 nM 5.80
CHEMBL5574727 IC50 = 1580.0 nM 5.80