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Assay Detail

CHEMBL3995183

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

Binding
Inhibition of recombinant human GST-fused KDR kinase expressed in insect Sf21 cells using poly-Glu/Tyr (4:1) peptide as substrate
7
Total Activities
7
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

An insight on synthetic and medicinal aspects of pyrazolo[1,5-a]pyrimidine scaffold.
Cherukupalli S, Karpoormath R, Chandrasekaran B, Hampannavar GA, Thapliyal N, Palakollu VN.
Eur J Med Chem (2017) 126 : 298 -352
PubMed 27894044 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.77 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL333021 L-21649 1.0 1 8.52
CHEMBL324335 1 8.40
CHEMBL331465 1 8.05
CHEMBL4082186 1 7.72
CHEMBL4081227 1 7.62
CHEMBL96149 1 7.43
CHEMBL92279 1 6.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL333021 L-21649 IC50 = 3.0 nM 8.52
CHEMBL324335 IC50 = 4.0 nM 8.40
CHEMBL331465 IC50 = 9.0 nM 8.05
CHEMBL4082186 IC50 = 19.0 nM 7.72
CHEMBL4081227 IC50 = 24.0 nM 7.62
CHEMBL96149 IC50 = 37.0 nM 7.43
CHEMBL92279 IC50 = 224.0 nM 6.65