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Assay Detail

CHEMBL1670765

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Binding
Inhibition of human recombinant PDGFRalpha in cell free system after 60 mins
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Isosteric replacement of the Z-enone with haloethyl ketone and E-enone in a resorcylic acid lactone series and biological evaluation.
Napolitano C, Natoni A, Santocanale C, Evensen L, Lorens JB, Murphy PV.
Bioorg Med Chem Lett (2011) 21 : 1167 -1170
PubMed 21273066 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.49 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1668411 1 9.62
CHEMBL1668418 1 7.57
CHEMBL1668414 1 7.06
CHEMBL1668419 1 7.05
CHEMBL1651523 1 6.36
CHEMBL1668420 1 6.35
CHEMBL1668412 1 5.92
CHEMBL1668413 1 5.85
CHEMBL1668415 1 5.64
CHEMBL1668417 1 5.07
CHEMBL1668416 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1668411 IC50 = 0.24 nM 9.62
CHEMBL1668418 IC50 = 27.0 nM 7.57
CHEMBL1668414 IC50 = 87.0 nM 7.06
CHEMBL1668419 IC50 = 89.0 nM 7.05
CHEMBL1651523 IC50 = 440.0 nM 6.36
CHEMBL1668420 IC50 = 450.0 nM 6.35
CHEMBL1668412 IC50 = 1200.0 nM 5.92
CHEMBL1668413 IC50 = 1400.0 nM 5.85
CHEMBL1668415 IC50 = 2300.0 nM 5.64
CHEMBL1668417 IC50 = 8600.0 nM 5.07
CHEMBL1668416 IC50 = 14000.0 nM 4.85