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Assay Detail

CHEMBL764773

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

Binding
Inhibition of Platelet-derived growth factor receptor
10
Total Activities
10
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 10 6.92 7.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL107677 1 7.39
CHEMBL104477 1 7.19
CHEMBL104466 1 7.12
CHEMBL105066 1 7.04
CHEMBL104473 1 7.02
CHEMBL107402 1 6.91
CHEMBL104616 1 6.89
CHEMBL319435 1 6.80
CHEMBL106614 1 6.65
CHEMBL104798 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL107677 IC50 = 41.0 nM 7.39
CHEMBL104477 IC50 = 65.0 nM 7.19
CHEMBL104466 IC50 = 76.0 nM 7.12
CHEMBL105066 IC50 = 92.0 nM 7.04
CHEMBL104473 IC50 = 96.0 nM 7.02
CHEMBL107402 IC50 = 124.0 nM 6.91
CHEMBL104616 IC50 = 128.0 nM 6.89
CHEMBL319435 IC50 = 159.0 nM 6.80
CHEMBL106614 IC50 = 226.0 nM 6.65
CHEMBL104798 IC50 = 601.0 nM 6.22