Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL697304

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

Binding
Inhibition of human tie-2 kinase.
10
Total Activities
10
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

Angiopoietin-1 receptor (CHEMBL4128)
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 10 5.95 6.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL402673 1 6.86
CHEMBL47787 1 6.28
CHEMBL46785 1 6.22
CHEMBL46176 1 6.05
CHEMBL295528 1 6.04
CHEMBL45651 1 6.03
CHEMBL417006 1 5.84
CHEMBL295601 1 5.61
CHEMBL297363 1 5.33
CHEMBL45693 1 5.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL402673 IC50 = 137.0 nM 6.86
CHEMBL47787 IC50 = 521.0 nM 6.28
CHEMBL46785 IC50 = 606.0 nM 6.22
CHEMBL46176 IC50 = 888.0 nM 6.05
CHEMBL295528 IC50 = 910.0 nM 6.04
CHEMBL45651 IC50 = 933.0 nM 6.03
CHEMBL417006 IC50 = 1440.0 nM 5.84
CHEMBL295601 IC50 = 2450.0 nM 5.61
CHEMBL297363 IC50 = 4680.0 nM 5.33
CHEMBL45693 IC50 = 5730.0 nM 5.24