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Assay Detail

CHEMBL899826

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Binding
Inhibition of Tie2
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Angiopoietin-1 receptor (CHEMBL4128)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of triarylimidazoles for Tie2: influence of conformation on potency.
Johnson NW, Semones M, Adams JL, Hansbury M, Winkler J.
Bioorg Med Chem Lett (2007) 17 : 5514 -5517
PubMed 17826092 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.82 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL237570 1 7.92
CHEMBL2096892 1 7.66
CHEMBL236716 1 7.44
CHEMBL391891 1 7.40
CHEMBL236924 1 7.29
CHEMBL392332 1 7.23
CHEMBL399410 1 7.22
CHEMBL236503 1 7.11
CHEMBL236300 1 7.09
CHEMBL2448122 1 7.02
CHEMBL237571 1 6.94
CHEMBL236299 1 6.80
CHEMBL391890 1 6.60
CHEMBL391889 1 6.58
CHEMBL237359 1 6.47
CHEMBL236504 1 6.46
CHEMBL236686 1 6.41
CHEMBL236505 1 6.08
CHEMBL236715 1 5.89
CHEMBL236717 1 5.82
CHEMBL236298 1 5.80
CHEMBL237352 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL237570 IC50 = 12.0 nM 7.92
CHEMBL2096892 IC50 = 22.0 nM 7.66
CHEMBL236716 IC50 = 36.0 nM 7.44
CHEMBL391891 IC50 = 40.0 nM 7.40
CHEMBL236924 IC50 = 51.0 nM 7.29
CHEMBL392332 IC50 = 59.0 nM 7.23
CHEMBL399410 IC50 = 60.0 nM 7.22
CHEMBL236503 IC50 = 78.0 nM 7.11
CHEMBL236300 IC50 = 82.0 nM 7.09
CHEMBL2448122 IC50 = 95.0 nM 7.02
CHEMBL237571 IC50 = 114.0 nM 6.94
CHEMBL236299 IC50 = 157.0 nM 6.80
CHEMBL391890 IC50 = 250.0 nM 6.60
CHEMBL391889 IC50 = 260.0 nM 6.58
CHEMBL237359 IC50 = 335.0 nM 6.47
CHEMBL236504 IC50 = 346.0 nM 6.46
CHEMBL236686 IC50 = 387.0 nM 6.41
CHEMBL236505 IC50 = 836.0 nM 6.08
CHEMBL236715 IC50 = 1300.0 nM 5.89
CHEMBL236717 IC50 = 1500.0 nM 5.82
CHEMBL236298 IC50 = 1600.0 nM 5.80
CHEMBL237352 IC50 > 20000.0 nM -