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Assay Detail

CHEMBL765709

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Binding
Inhibition of Platelet-derived growth factor receptor
13
Total Activities
13
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 2: the synthesis and biological activities of RPR127963 an orally bioavailable inhibitor.
He W, Myers MR, Hanney B, Spada AP, Bilder G, Galzcinski H, Amin D, Needle S, Page K, Jayyosi Z, Perrone MH.
Bioorg Med Chem Lett (2003) 13 : 3097 -3100
PubMed 12941342 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.03 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL105364 1 8.22
CHEMBL104266 1 7.75
CHEMBL105322 1 7.62
CHEMBL2111669 1 7.55
CHEMBL107677 1 7.39
CHEMBL321276 1 7.31
CHEMBL104074 1 7.17
CHEMBL104466 1 7.12
CHEMBL107402 1 6.91
CHEMBL2112462 1 6.46
CHEMBL66643 1 6.34
CHEMBL106878 1 6.03
CHEMBL104581 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL105364 IC50 = 6.0 nM 8.22
CHEMBL104266 IC50 = 18.0 nM 7.75
CHEMBL105322 IC50 = 24.0 nM 7.62
CHEMBL2111669 IC50 = 28.0 nM 7.55
CHEMBL107677 IC50 = 41.0 nM 7.39
CHEMBL321276 IC50 = 49.0 nM 7.31
CHEMBL104074 IC50 = 68.0 nM 7.17
CHEMBL104466 IC50 = 76.0 nM 7.12
CHEMBL107402 IC50 = 124.0 nM 6.91
CHEMBL2112462 IC50 = 345.0 nM 6.46
CHEMBL66643 IC50 = 461.0 nM 6.34
CHEMBL106878 IC50 = 930.0 nM 6.03
CHEMBL104581 IC50 = 3100.0 nM 5.51