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Assay Detail

CHEMBL1002019

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

Binding
Inhibition of VEGFR2 by HTRF assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Vascular endothelial growth factor receptor 2 (CHEMBL279)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of pyrazolo[1,5-b]pyridazines as selective cyclin dependent kinase inhibitors.
Stevens KL, Reno MJ, Alberti JB, Price DJ, Kane-Carson LS, Knick VB, Shewchuk LM, Hassell AM, Veal JM, Davis ST, Griffin RJ, Peel MR.
Bioorg Med Chem Lett (2008) 18 : 5758 -5758
PubMed 18835709 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.58 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL496575 1 7.60
CHEMBL524086 1 7.20
CHEMBL496360 1 7.20
CHEMBL495545 1 6.40
CHEMBL495544 1 5.60
CHEMBL524057 GW683768X 1 5.50
CHEMBL525194 1 -
CHEMBL498625 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL496575 IC50 = 25.0 nM 7.60
CHEMBL524086 IC50 = 63.0 nM 7.20
CHEMBL496360 IC50 = 63.0 nM 7.20
CHEMBL495545 IC50 = 400.0 nM 6.40
CHEMBL495544 IC50 = 2500.0 nM 5.60
CHEMBL524057 GW683768X IC50 = 3200.0 nM 5.50
CHEMBL525194 IC50 > 20000.0 nM -
CHEMBL498625 IC50 > 20000.0 nM -