Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL770479

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

Binding
Inhibition of Platelet-derived growth factor receptor (PDGFr) tyrosine kinase in rat aortic vascular smooth muscle cells (RAVSMCs).
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors.
Hamby JM, Connolly CJ, Schroeder MC, Winters RT, Showalter HD, Panek RL, Major TC, Olsewski B, Ryan MJ, Dahring T, Lu GH, Keiser J, Amar A, Shen C, Kraker AJ, Slintak V, Nelson JM, Fry DW, Bradford L, Hallak H, Doherty AM.
J Med Chem (1997) 40 : 2296 -2303
PubMed 9240345 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.17 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301483 1 6.72
CHEMBL45827 1 6.51
CHEMBL57323 1 6.47
CHEMBL57347 1 6.33
CHEMBL299026 1 6.18
CHEMBL57366 1 5.96
CHEMBL432738 1 5.89
CHEMBL76599 1 5.33
CHEMBL75188 1 -
CHEMBL299763 1 -
CHEMBL56236 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL301483 IC50 = 190.0 nM 6.72
CHEMBL45827 IC50 = 310.0 nM 6.51
CHEMBL57323 IC50 = 340.0 nM 6.47
CHEMBL57347 IC50 = 470.0 nM 6.33
CHEMBL299026 IC50 = 660.0 nM 6.18
CHEMBL57366 IC50 = 1110.0 nM 5.96
CHEMBL432738 IC50 = 1300.0 nM 5.89
CHEMBL76599 IC50 = 4670.0 nM 5.33
CHEMBL75188 IC50 > 50000.0 nM -
CHEMBL299763 IC50 > 50000.0 nM -
CHEMBL56236 IC50 > 50000.0 nM -