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Assay Detail

CHEMBL770474

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

Binding
Inhibition of PDGF-stimulated Platelet-derived growth factor receptor autophosphorylation in C6 rat glioma cells after 2 hr
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type C6
Confidence 5 — Multiple protein complex / RNA
Curated By Expert

Target

Platelet-derived growth factor receptor (PDGFr) (CHEMBL2111344)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Synthesis and tyrosine kinase inhibitory activity of a series of 2-amino-8H-pyrido[2,3-d]pyrimidines: identification of potent, selective platelet-derived growth factor receptor tyrosine kinase inhibitors.
Boschelli DH, Wu Z, Klutchko SR, Showalter HD, Hamby JM, Lu GH, Major TC, Dahring TK, Batley B, Panek RL, Keiser J, Hartl BG, Kraker AJ, Klohs WD, Roberts BJ, Patmore S, Elliott WL, Steinkampf R, Bradford LA, Hallak H, Doherty AM.
J Med Chem (1998) 41 : 4365 -4377
PubMed 9784112 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.88 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL134851 1 8.52
CHEMBL136106 1 7.24
CHEMBL434448 1 -
CHEMBL342475 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL134851 IC50 = 3.0 nM 8.52
CHEMBL136106 IC50 = 58.0 nM 7.24
CHEMBL434448 IC50 > 25.0 nM -
CHEMBL342475 IC50 > 25.0 nM -