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Assay Detail

CHEMBL2024778

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

Binding
Inhibition of human KDR phosphorylation expressed in mouse NIH3T3 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type NIH3T3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.
Curtin ML, Frey RR, Heyman HR, Soni NB, Marcotte PA, Pease LJ, Glaser KB, Magoc TJ, Tapang P, Albert DH, Osterling DJ, Olson AM, Bouska JJ, Guan Z, Preusser LC, Polakowski JS, Stewart KD, Tse C, Davidsen SK, Michaelides MR.
Bioorg Med Chem Lett (2012) 22 : 3208 -3212
PubMed 22465635 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.03 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2023221 1 9.00
CHEMBL2021941 1 9.00
CHEMBL2023224 1 8.52
CHEMBL1979883 1 8.10
CHEMBL2023222 1 7.85
CHEMBL1969102 1 7.85
CHEMBL1967116 1 7.85
CHEMBL2023220 1 7.66
CHEMBL2023223 1 7.51
CHEMBL394619 1 7.50
CHEMBL231511 1 7.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2023221 IC50 = 1.0 nM 9.00
CHEMBL2021941 IC50 = 1.0 nM 9.00
CHEMBL2023224 IC50 = 3.0 nM 8.52
CHEMBL1979883 IC50 = 8.0 nM 8.10
CHEMBL2023222 IC50 = 14.0 nM 7.85
CHEMBL1969102 IC50 = 14.0 nM 7.85
CHEMBL1967116 IC50 = 14.0 nM 7.85
CHEMBL2023220 IC50 = 22.0 nM 7.66
CHEMBL2023223 IC50 = 31.0 nM 7.51
CHEMBL394619 IC50 = 32.0 nM 7.50
CHEMBL231511 IC50 = 33.0 nM 7.48