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Assay Detail

CHEMBL764770

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

Binding
Inhibition of Platelet-derived growth factor receptor
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 1: SAR exploration and effective bioisosteric replacement of a phenyl substituent.
Myers MR, He W, Hanney B, Setzer N, Maguire MP, Zulli A, Bilder G, Galzcinski H, Amin D, Needle S, Spada AP.
Bioorg Med Chem Lett (2003) 13 : 3091 -3095
PubMed 12941341 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.84 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL322028 1 8.40
CHEMBL105364 1 8.22
CHEMBL104087 1 7.38
CHEMBL108216 1 6.47
CHEMBL66643 1 6.34
CHEMBL105305 1 5.80
CHEMBL322428 1 5.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL322028 IC50 = 4.0 nM 8.40
CHEMBL105364 IC50 = 6.0 nM 8.22
CHEMBL104087 IC50 = 42.0 nM 7.38
CHEMBL108216 IC50 = 340.0 nM 6.47
CHEMBL66643 IC50 = 461.0 nM 6.34
CHEMBL105305 IC50 = 1600.0 nM 5.80
CHEMBL322428 IC50 = 5100.0 nM 5.29