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Assay Detail

CHEMBL768950

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Functional
Inhibition of Platelet-derived growth factor induced 3T3 cell proliferation
13
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type 3T3
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Platelet-derived growth factor receptor (CHEMBL2096980)
Type PROTEIN COMPLEX
Organism Mus musculus

Publication

Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase.
Sun L, Liang C, Shirazian S, Zhou Y, Miller T, Cui J, Fukuda JY, Chu JY, Nematalla A, Wang X, Chen H, Sistla A, Luu TC, Tang F, Wei J, Tang C.
J Med Chem (2003) 46 : 1116 -1119
PubMed 12646019 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.67 8.00
NT 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL535 SUNITINIB 4.0 1 8.00
CHEMBL13983 1 7.70
CHEMBL268731 1 7.00
CHEMBL13485 SU-11652 1 7.00
CHEMBL13629 1 7.00
CHEMBL13608 TOCERANIB 2.0 1 7.00
CHEMBL13976 1 7.00
CHEMBL274654 ORANTINIB 3.0 1 6.00
CHEMBL267293 1 6.00
CHEMBL275117 1 6.00
CHEMBL276711 SEMAXANIB 3.0 1 4.69
CHEMBL430155 1 -
CHEMBL13354 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL535 SUNITINIB IC50 = 10.0 nM 8.00
CHEMBL13983 IC50 = 20.0 nM 7.70
CHEMBL268731 IC50 = 100.0 nM 7.00
CHEMBL13485 SU-11652 IC50 = 100.0 nM 7.00
CHEMBL13629 IC50 = 100.0 nM 7.00
CHEMBL13608 TOCERANIB IC50 = 100.0 nM 7.00
CHEMBL13976 IC50 = 100.0 nM 7.00
CHEMBL274654 ORANTINIB IC50 = 1000.0 nM 6.00
CHEMBL267293 IC50 = 1000.0 nM 6.00
CHEMBL275117 IC50 = 1000.0 nM 6.00
CHEMBL276711 SEMAXANIB IC50 = 20300.0 nM 4.69
CHEMBL430155 NT - -
CHEMBL13354 IC50 = - nM -