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Assay Detail

CHEMBL700241

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Binding
Tested in vitro for inhibition of KDR-receptor tyrosine kinase
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Vascular endothelial growth factor receptor 2 (CHEMBL279)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Substituted 5,7-diphenyl-pyrrolo[2,3d]pyrimidines: potent inhibitors of the tyrosine kinase c-Src.
Missbach M, Altmann E, Widler L, Susa M, Buchdunger E, Mett H, Meyer T, Green J.
Bioorg Med Chem Lett (2000) 10 : 945 -949
PubMed 10853665 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.10 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL176705 1 6.70
CHEMBL169757 1 6.30
CHEMBL367442 1 6.22
CHEMBL176309 1 6.00
CHEMBL369014 1 5.96
CHEMBL176702 1 5.44
CHEMBL172973 1 -
CHEMBL105436 1 -
CHEMBL175409 1 -
CHEMBL176815 1 -
CHEMBL424375 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL176705 IC50 = 200.0 nM 6.70
CHEMBL169757 IC50 = 500.0 nM 6.30
CHEMBL367442 IC50 = 600.0 nM 6.22
CHEMBL176309 IC50 = 1000.0 nM 6.00
CHEMBL369014 IC50 = 1100.0 nM 5.96
CHEMBL176702 IC50 = 3600.0 nM 5.44
CHEMBL172973 IC50 > 1000.0 nM -
CHEMBL105436 IC50 > 1000.0 nM -
CHEMBL175409 IC50 > 1000.0 nM -
CHEMBL176815 IC50 > 1000.0 nM -
CHEMBL424375 IC50 > 1000.0 nM -