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Assay Detail

CHEMBL809315

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Binding
Inhibition of TIE-2 kinase
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.
Calderwood DJ, Johnston DN, Munschauer R, Rafferty P.
Bioorg Med Chem Lett (2002) 12 : 1683 -1686
PubMed 12039590 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.20 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL47203 1 6.60
CHEMBL48554 1 5.29
CHEMBL296534 1 5.18
CHEMBL296103 1 4.93
CHEMBL431342 1 4.92
CHEMBL297359 1 4.78
CHEMBL47202 1 4.67
CHEMBL416444 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL47203 IC50 = 250.0 nM 6.60
CHEMBL48554 IC50 = 5150.0 nM 5.29
CHEMBL296534 IC50 = 6620.0 nM 5.18
CHEMBL296103 IC50 = 11620.0 nM 4.93
CHEMBL431342 IC50 = 12160.0 nM 4.92
CHEMBL297359 IC50 = 16710.0 nM 4.78
CHEMBL47202 IC50 = 21380.0 nM 4.67
CHEMBL416444 IC50 > 50000.0 nM -