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Assay Detail

CHEMBL829592

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

Binding
Inhibition of human Vascular endothelial growth factor receptor 2
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 Expert

Target

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

Publication

Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.
Harris PA, Cheung M, Hunter RN, Brown ML, Veal JM, Nolte RT, Wang L, Liu W, Crosby RM, Johnson JH, Epperly AH, Kumar R, Luttrell DK, Stafford JA.
J Med Chem (2005) 48 : 1610 -1619
PubMed 15743202 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 6.96 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL24828 VANDETANIB 4.0 1 8.05
CHEMBL194939 1 7.82
CHEMBL193609 1 7.80
CHEMBL190872 1 7.75
CHEMBL178507 1 7.66
CHEMBL194176 1 7.66
CHEMBL275473 GW572401X 1 7.64
CHEMBL365815 1 7.60
CHEMBL193955 1 7.54
CHEMBL191993 1 7.41
CHEMBL369751 1 7.30
CHEMBL370744 1 7.29
CHEMBL193386 1 7.12
CHEMBL195237 1 7.11
CHEMBL194883 1 7.10
CHEMBL364082 1 7.10
CHEMBL364259 1 7.09
CHEMBL191779 1 7.06
CHEMBL372474 GW678313X 1 7.05
CHEMBL191705 GW621431X 1 7.04
CHEMBL179465 GW621970X 1 7.03
CHEMBL443563 GW627512B 1 7.00
CHEMBL361642 1 6.85
CHEMBL1794060 GW575533A 1 6.85
CHEMBL101253 VATALANIB 3.0 1 6.80
CHEMBL176553 GW631581B 1 6.77
CHEMBL179311 GW580509X 1 6.44
CHEMBL179453 GW622055X 1 6.44
CHEMBL1794062 GW577921A 1 6.42
CHEMBL194062 GW572399X 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL24828 VANDETANIB IC50 = 9.0 nM 8.05
CHEMBL194939 IC50 = 15.0 nM 7.82
CHEMBL193609 IC50 = 16.0 nM 7.80
CHEMBL190872 IC50 = 18.0 nM 7.75
CHEMBL178507 IC50 = 22.0 nM 7.66
CHEMBL194176 IC50 = 22.0 nM 7.66
CHEMBL275473 GW572401X IC50 = 23.0 nM 7.64
CHEMBL365815 IC50 = 25.0 nM 7.60
CHEMBL193955 IC50 = 29.0 nM 7.54
CHEMBL191993 IC50 = 39.0 nM 7.41
CHEMBL369751 IC50 = 50.0 nM 7.30
CHEMBL370744 IC50 = 51.0 nM 7.29
CHEMBL193386 IC50 = 76.0 nM 7.12
CHEMBL195237 IC50 = 78.0 nM 7.11
CHEMBL364082 IC50 = 79.0 nM 7.10
CHEMBL194883 IC50 = 79.0 nM 7.10
CHEMBL364259 IC50 = 81.0 nM 7.09
CHEMBL191779 IC50 = 87.0 nM 7.06
CHEMBL372474 GW678313X IC50 = 89.0 nM 7.05
CHEMBL191705 GW621431X IC50 = 91.0 nM 7.04
CHEMBL179465 GW621970X IC50 = 93.0 nM 7.03
CHEMBL443563 GW627512B IC50 = 100.0 nM 7.00
CHEMBL361642 IC50 = 141.0 nM 6.85
CHEMBL1794060 GW575533A IC50 = 140.0 nM 6.85
CHEMBL101253 VATALANIB IC50 = 160.0 nM 6.80
CHEMBL176553 GW631581B IC50 = 170.0 nM 6.77
CHEMBL179311 GW580509X IC50 = 360.0 nM 6.44
CHEMBL179453 GW622055X IC50 = 360.0 nM 6.44
CHEMBL1794062 GW577921A IC50 = 380.0 nM 6.42
CHEMBL194062 GW572399X IC50 = 500.0 nM 6.30
CHEMBL194113 IC50 = 500.0 nM 6.30
CHEMBL371374 IC50 = 720.0 nM 6.14
CHEMBL192417 GW632046X IC50 = 870.0 nM 6.06
CHEMBL193912 IC50 = 870.0 nM 6.06
CHEMBL1794061 GW627834A IC50 = 930.0 nM 6.03
CHEMBL318728 GW549390X IC50 = 1200.0 nM 5.92
CHEMBL191626 IC50 = 1410.0 nM 5.85
CHEMBL194117 IC50 > 10000.0 nM -