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Assay Detail

CHEMBL4256562

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

Binding
Inhibition of recombinant mouse N-terminal FLAG-tagged Notch1 (1704 to 2531 residues) expressed in human LS174T cells assessed as reduction in doxycycline-induced NICD expression after 12 hrs by Bright-Glo luciferase reporter gene assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type LS174T
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Neurogenic locus notch homolog protein 1 (CHEMBL4295799)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

The Notch Inhibitors Isolated from Nerium indicum.
Arai MA, Akamine R, Hayashi N, Koyano T, Kowithayakorn T, Ishibashi M.
J Nat Prod (2018) 81 : 1235 -1240
PubMed 29693393 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.81 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4285883 OLEANDRIN 1.0 1 6.92
CHEMBL4292704 1 5.60
CHEMBL229258 1 5.57
CHEMBL4282921 1 5.57
CHEMBL229259 1 5.38
CHEMBL4284834 1 -
CHEMBL1453 DIGITOXIGENIN 1 -
CHEMBL229260 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4285883 OLEANDRIN IC50 = 120.0 nM 6.92
CHEMBL4292704 IC50 = 2500.0 nM 5.60
CHEMBL229258 IC50 = 2700.0 nM 5.57
CHEMBL4282921 IC50 = 2700.0 nM 5.57
CHEMBL229259 IC50 = 4200.0 nM 5.38
CHEMBL4284834 IC50 - -
CHEMBL1453 DIGITOXIGENIN IC50 - -
CHEMBL229260 IC50 - -