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Assay Detail

CHEMBL860933

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Functional
Inhibition of PDGFR alpha phosphorylation in G292 cell
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type G292
Confidence 9 — Direct single protein target
Curated By Expert

Target

Platelet-derived growth factor receptor alpha (CHEMBL2007)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of potent and selective inhibitors of PDGF receptor autophosphorylation.
Furuta T, Sakai T, Senga T, Osawa T, Kubo K, Shimizu T, Suzuki R, Yoshino T, Endo M, Miwa A.
J Med Chem (2006) 49 : 2186 -2192
PubMed 16570914 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.87 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL203227 1 8.40
CHEMBL202919 1 8.30
CHEMBL380703 1 8.30
CHEMBL203279 1 8.22
CHEMBL425935 1 8.22
CHEMBL205089 1 8.15
CHEMBL378489 1 8.10
CHEMBL204225 1 8.05
CHEMBL205953 1 7.92
CHEMBL204120 1 7.82
CHEMBL425043 1 7.75
CHEMBL205372 1 7.55
CHEMBL382399 1 7.43
CHEMBL205674 1 7.40
CHEMBL204409 1 7.34
CHEMBL941 IMATINIB 4.0 1 7.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL203227 IC50 = 4.0 nM 8.40
CHEMBL202919 IC50 = 5.0 nM 8.30
CHEMBL380703 IC50 = 5.0 nM 8.30
CHEMBL203279 IC50 = 6.0 nM 8.22
CHEMBL425935 IC50 = 6.0 nM 8.22
CHEMBL205089 IC50 = 7.0 nM 8.15
CHEMBL378489 IC50 = 8.0 nM 8.10
CHEMBL204225 IC50 = 9.0 nM 8.05
CHEMBL205953 IC50 = 12.0 nM 7.92
CHEMBL204120 IC50 = 15.0 nM 7.82
CHEMBL425043 IC50 = 18.0 nM 7.75
CHEMBL205372 IC50 = 28.0 nM 7.55
CHEMBL382399 IC50 = 37.0 nM 7.43
CHEMBL205674 IC50 = 40.0 nM 7.40
CHEMBL204409 IC50 = 46.0 nM 7.34
CHEMBL941 IMATINIB IC50 = 96.0 nM 7.02