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Assay Detail

CHEMBL828722

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

Binding
Inhibition of baculovirus expressed human VEGFR2
7
Total Activities
7
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

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

Publication

Synthesis, modeling, and in vitro activity of (3'S)-epi-K-252a analogues. Elucidating the stereochemical requirements of the 3'-sugar alcohol on trkA tyrosine kinase activity.
Gingrich DE, Yang SX, Gessner GW, Angeles TS, Hudkins RL.
J Med Chem (2005) 48 : 3776 -3783
PubMed 15916429 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.54 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370493 1 8.40
CHEMBL2113063 1 7.96
CHEMBL94678 1 7.72
CHEMBL281948 K-252A 1 7.37
CHEMBL365585 1 7.19
CHEMBL2113062 1 7.12
CHEMBL2113065 1 7.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370493 IC50 = 4.0 nM 8.40
CHEMBL2113063 IC50 = 11.0 nM 7.96
CHEMBL94678 IC50 = 19.0 nM 7.72
CHEMBL281948 K-252A IC50 = 43.0 nM 7.37
CHEMBL365585 IC50 = 65.0 nM 7.19
CHEMBL2113062 IC50 = 76.0 nM 7.12
CHEMBL2113065 IC50 = 90.0 nM 7.05