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Assay Detail

CHEMBL951786

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

Binding
Inhibition of PDGFR autophosphorylation in mouse Swiss 3T3 fibroblast by immunoblotting
30
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Inhibition of PDGFR tyrosine kinase activity by a series of novel N-(3-(4-(pyridin-3-yl)-1H-imidazol-2-ylamino)phenyl)amides: a SAR study on the bioisosterism of pyrimidine and imidazole.
Mahboobi S, Sellmer A, Eswayah A, Elz S, Uecker A, Böhmer FD.
Eur J Med Chem (2008) 43 : 1444 -1453
PubMed 17983688 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 5.98 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20926 1 7.00
CHEMBL473116 1 6.70
CHEMBL462643 2 6.70
CHEMBL462626 1 6.52
CHEMBL941 IMATINIB 4.0 1 6.52
CHEMBL474525 1 6.52
CHEMBL472921 1 6.52
CHEMBL516043 1 6.40
CHEMBL523953 1 6.22
CHEMBL514457 1 6.22
CHEMBL516222 1 5.80
CHEMBL473115 1 5.75
CHEMBL473322 1 5.66
CHEMBL514458 1 5.33
CHEMBL462625 1 5.23
CHEMBL473321 1 5.19
CHEMBL474526 1 5.19
CHEMBL517443 1 5.15
CHEMBL423288 1 4.30
CHEMBL472920 1 -
CHEMBL472926 1 -
CHEMBL462444 1 -
CHEMBL517752 1 -
CHEMBL461740 1 -
CHEMBL472927 1 -
CHEMBL462642 1 -
CHEMBL461927 1 -
CHEMBL461926 1 -
CHEMBL473123 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20926 IC50 = 100.0 nM 7.00
CHEMBL462643 IC50 = 200.0 nM 6.70
CHEMBL462643 IC50 = 200.0 nM 6.70
CHEMBL473116 IC50 = 200.0 nM 6.70
CHEMBL462626 IC50 = 300.0 nM 6.52
CHEMBL941 IMATINIB IC50 = 300.0 nM 6.52
CHEMBL474525 IC50 = 300.0 nM 6.52
CHEMBL472921 IC50 = 300.0 nM 6.52
CHEMBL516043 IC50 = 400.0 nM 6.40
CHEMBL523953 IC50 = 600.0 nM 6.22
CHEMBL514457 IC50 = 600.0 nM 6.22
CHEMBL516222 IC50 = 1600.0 nM 5.80
CHEMBL473115 IC50 = 1800.0 nM 5.75
CHEMBL473322 IC50 = 2200.0 nM 5.66
CHEMBL514458 IC50 = 4700.0 nM 5.33
CHEMBL462625 IC50 = 5900.0 nM 5.23
CHEMBL473321 IC50 = 6500.0 nM 5.19
CHEMBL474526 IC50 = 6500.0 nM 5.19
CHEMBL517443 IC50 = 7100.0 nM 5.15
CHEMBL423288 IC50 = 50000.0 nM 4.30
CHEMBL472920 IC50 > 30000.0 nM -
CHEMBL473123 IC50 > 30000.0 nM -
CHEMBL472927 IC50 > 10000.0 nM -
CHEMBL472926 IC50 > 30000.0 nM -
CHEMBL462444 IC50 > 10000.0 nM -
CHEMBL517752 IC50 > 10000.0 nM -
CHEMBL462642 IC50 > 10000.0 nM -
CHEMBL461927 IC50 > 10000.0 nM -
CHEMBL461926 IC50 > 10000.0 nM -
CHEMBL461740 IC50 > 30000.0 nM -