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Assay Detail

CHEMBL930118

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

Binding
Inhibition of VEGF-induced human KDR phosphorylation in mouse 3T3 cells
29
Total Activities
29
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

Identification of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted kinase inhibitors.
Dai Y, Hartandi K, Soni NB, Pease LJ, Reuter DR, Olson AM, Osterling DJ, Doktor SZ, Albert DH, Bouska JJ, Glaser KB, Marcotte PA, Stewart KD, Davidsen SK, Michaelides MR.
Bioorg Med Chem Lett (2008) 18 : 386 -390
PubMed 18023347 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 8.31 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL272938 1 9.22
CHEMBL404669 1 9.15
CHEMBL257479 1 9.00
CHEMBL255743 1 9.00
CHEMBL271441 1 9.00
CHEMBL255744 1 8.96
CHEMBL273187 1 8.92
CHEMBL256246 1 8.89
CHEMBL255746 1 8.82
CHEMBL404367 1 8.74
CHEMBL257292 1 8.66
CHEMBL255955 1 8.59
CHEMBL402846 1 8.52
CHEMBL404342 1 8.51
CHEMBL403439 1 8.42
CHEMBL256043 1 8.41
CHEMBL404223 1 8.40
CHEMBL256205 1 8.29
CHEMBL403402 1 8.10
CHEMBL258141 1 8.09
CHEMBL404366 1 8.06
CHEMBL256824 1 7.89
CHEMBL255956 1 7.80
CHEMBL439068 1 7.47
CHEMBL257533 1 7.43
CHEMBL256825 1 7.34
CHEMBL404257 1 7.21
CHEMBL272767 1 7.19
CHEMBL404571 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL272938 IC50 = 0.6 nM 9.22
CHEMBL404669 IC50 = 0.7 nM 9.15
CHEMBL257479 IC50 = 1.0 nM 9.00
CHEMBL255743 IC50 = 1.0 nM 9.00
CHEMBL271441 IC50 = 1.0 nM 9.00
CHEMBL255744 IC50 = 1.1 nM 8.96
CHEMBL273187 IC50 = 1.2 nM 8.92
CHEMBL256246 IC50 = 1.3 nM 8.89
CHEMBL255746 IC50 = 1.5 nM 8.82
CHEMBL404367 IC50 = 1.8 nM 8.74
CHEMBL257292 IC50 = 2.2 nM 8.66
CHEMBL255955 IC50 = 2.6 nM 8.59
CHEMBL402846 IC50 = 3.0 nM 8.52
CHEMBL404342 IC50 = 3.1 nM 8.51
CHEMBL403439 IC50 = 3.8 nM 8.42
CHEMBL256043 IC50 = 3.9 nM 8.41
CHEMBL404223 IC50 = 4.0 nM 8.40
CHEMBL256205 IC50 = 5.1 nM 8.29
CHEMBL403402 IC50 = 7.9 nM 8.10
CHEMBL258141 IC50 = 8.1 nM 8.09
CHEMBL404366 IC50 = 8.8 nM 8.06
CHEMBL256824 IC50 = 13.0 nM 7.89
CHEMBL255956 IC50 = 16.0 nM 7.80
CHEMBL439068 IC50 = 34.0 nM 7.47
CHEMBL257533 IC50 = 37.0 nM 7.43
CHEMBL256825 IC50 = 46.0 nM 7.34
CHEMBL404257 IC50 = 61.0 nM 7.21
CHEMBL272767 IC50 = 65.0 nM 7.19
CHEMBL404571 IC50 = 99.0 nM 7.00