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Assay Detail

CHEMBL761271

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

Binding
Inhibition of Platelet-derived growth factor receptor tyrosine kinase
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Platelet-derived growth factor receptor (CHEMBL2095189)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

5,7-Dimethoxy-3-(4-pyridinyl)quinoline is a potent and selective inhibitor of human vascular beta-type platelet-derived growth factor receptor tyrosine kinase.
Dolle RE, Dunn JA, Bobko M, Singh B, Kuster JE, Baizman E, Harris AL, Sawutz DG, Miller D, Wang S.
J Med Chem (1994) 37 : 2627 -2629
PubMed 8064792 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.04 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68423 1 7.10
CHEMBL86664 1 6.52
CHEMBL280069 1 6.52
CHEMBL90780 1 6.40
CHEMBL86717 1 6.40
CHEMBL329622 1 6.22
CHEMBL87083 1 5.89
CHEMBL89550 1 5.82
CHEMBL314811 1 5.04
CHEMBL87084 1 4.44
CHEMBL313235 1 -
CHEMBL89115 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68423 IC50 = 80.0 nM 7.10
CHEMBL86664 IC50 = 300.0 nM 6.52
CHEMBL280069 IC50 = 300.0 nM 6.52
CHEMBL90780 IC50 = 400.0 nM 6.40
CHEMBL86717 IC50 = 400.0 nM 6.40
CHEMBL329622 IC50 = 600.0 nM 6.22
CHEMBL87083 IC50 = 1300.0 nM 5.89
CHEMBL89550 IC50 = 1500.0 nM 5.82
CHEMBL314811 IC50 = 9200.0 nM 5.04
CHEMBL87084 IC50 = 36000.0 nM 4.44
CHEMBL313235 IC50 > 50000.0 nM -
CHEMBL89115 IC50 > 50000.0 nM -