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Assay Detail

CHEMBL847682

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Binding
Inhibition of tie-2 at 5 uM ATP
11
Total Activities
11
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

Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I.
Arnold LD, Calderwood DJ, Dixon RW, Johnston DN, Kamens JS, Munschauer R, Rafferty P, Ratnofsky SE.
Bioorg Med Chem Lett (2000) 10 : 2167 -2170
PubMed 11012021 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.80 7.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL69129 1 7.23
CHEMBL69827 1 6.82
CHEMBL307982 1 6.37
CHEMBL419082 1 6.22
CHEMBL47940 1 5.70
CHEMBL302281 1 5.57
CHEMBL69638 1 5.47
CHEMBL68774 1 5.31
CHEMBL306380 1 5.16
CHEMBL306012 1 5.16
CHEMBL304760 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL69129 IC50 = 58.3 nM 7.23
CHEMBL69827 IC50 = 150.0 nM 6.82
CHEMBL307982 IC50 = 430.0 nM 6.37
CHEMBL419082 IC50 = 600.0 nM 6.22
CHEMBL47940 IC50 = 1980.0 nM 5.70
CHEMBL302281 IC50 = 2680.0 nM 5.57
CHEMBL69638 IC50 = 3400.0 nM 5.47
CHEMBL68774 IC50 = 4900.0 nM 5.31
CHEMBL306380 IC50 = 7000.0 nM 5.16
CHEMBL306012 IC50 = 7000.0 nM 5.16
CHEMBL304760 IC50 = 17870.0 nM 4.75