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Assay Detail

CHEMBL864250

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

Binding
Inhibition of TIE2
5
Total Activities
5
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

Isothiazolopyrimidines and isoxazolopyrimidines as novel multi-targeted inhibitors of receptor tyrosine kinases.
Ji Z, Ahmed AA, Albert DH, Bouska JJ, Bousquet PF, Cunha GA, Glaser KB, Guo J, Li J, Marcotte PA, Moskey MD, Pease LJ, Stewart KD, Yates M, Davidsen SK, Michaelides MR.
Bioorg Med Chem Lett (2006) 16 : 4326 -4330
PubMed 16735117 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.09 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL262433 1 7.72
CHEMBL214258 1 7.66
CHEMBL213504 1 7.55
CHEMBL376951 1 6.38
CHEMBL196363 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL262433 IC50 = 19.0 nM 7.72
CHEMBL214258 IC50 = 22.0 nM 7.66
CHEMBL213504 IC50 = 28.0 nM 7.55
CHEMBL376951 IC50 = 415.0 nM 6.38
CHEMBL196363 IC50 = 730.0 nM 6.14