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Assay Detail

CHEMBL764645

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

Binding
Inhibition of PDGF- beta receptor kinase
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Platelet-derived growth factor receptor beta (CHEMBL1913)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis.
Bold G, Altmann KH, Frei J, Lang M, Manley PW, Traxler P, Wietfeld B, Brüggen J, Buchdunger E, Cozens R, Ferrari S, Furet P, Hofmann F, Martiny-Baron G, Mestan J, Rösel J, Sills M, Stover D, Acemoglu F, Boss E, Emmenegger R, Lässer L, Masso E, Roth R, Schlachter C, Vetterli W.
J Med Chem (2000) 43 : 2310 -2323
PubMed 10882357 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.84 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL75232 1 6.22
CHEMBL75196 1 6.22
CHEMBL74197 1 6.10
CHEMBL75462 1 6.10
CHEMBL78303 1 6.00
CHEMBL309331 1 5.85
CHEMBL75034 1 5.70
CHEMBL431006 1 5.70
CHEMBL74587 1 5.55
CHEMBL77555 1 5.40
CHEMBL306295 1 5.40
CHEMBL77933 1 -
CHEMBL74646 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL75232 IC50 = 600.0 nM 6.22
CHEMBL75196 IC50 = 600.0 nM 6.22
CHEMBL74197 IC50 = 800.0 nM 6.10
CHEMBL75462 IC50 = 800.0 nM 6.10
CHEMBL78303 IC50 = 1000.0 nM 6.00
CHEMBL309331 IC50 = 1400.0 nM 5.85
CHEMBL75034 IC50 = 2000.0 nM 5.70
CHEMBL431006 IC50 = 2000.0 nM 5.70
CHEMBL74587 IC50 = 2800.0 nM 5.55
CHEMBL77555 IC50 = 4000.0 nM 5.40
CHEMBL306295 IC50 = 4000.0 nM 5.40
CHEMBL77933 IC50 > 10000.0 nM -
CHEMBL74646 IC50 > 10000.0 nM -