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Assay Detail

CHEMBL698970

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

Binding
Inhibition of human VEGF-receptor 2 (kdr) kinase.
12
Total Activities
12
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

Pyrazolo[3,4-d]pyrimidines containing an extended 3-substituent as potent inhibitors of Lck -- a selectivity insight.
Burchat AF, Calderwood DJ, Friedman MM, Hirst GC, Li B, Rafferty P, Ritter K, Skinner BS.
Bioorg Med Chem Lett (2002) 12 : 1687 -1690
PubMed 12039591 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.46 6.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45651 1 6.58
CHEMBL45683 1 6.36
CHEMBL46785 1 5.42
CHEMBL47787 1 4.47
CHEMBL295528 1 4.46
CHEMBL416091 1 -
CHEMBL297363 1 -
CHEMBL417006 1 -
CHEMBL45693 1 -
CHEMBL43773 1 -
CHEMBL295601 1 -
CHEMBL402673 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45651 IC50 = 263.0 nM 6.58
CHEMBL45683 IC50 = 435.0 nM 6.36
CHEMBL46785 IC50 = 3810.0 nM 5.42
CHEMBL47787 IC50 = 34200.0 nM 4.47
CHEMBL295528 IC50 = 34600.0 nM 4.46
CHEMBL416091 IC50 > 50000.0 nM -
CHEMBL297363 IC50 > 50000.0 nM -
CHEMBL417006 IC50 > 50000.0 nM -
CHEMBL45693 IC50 > 50000.0 nM -
CHEMBL43773 IC50 > 50000.0 nM -
CHEMBL295601 IC50 > 50000.0 nM -
CHEMBL402673 IC50 > 50000.0 nM -