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Assay Detail

CHEMBL4132673

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
16
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type LS174T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neurogenic locus notch homolog protein 1 (CHEMBL2146346)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Notch Inhibitors from Calotropis gigantea That Induce Neuronal Differentiation of Neural Stem Cells.
Yoneyama T, Arai MA, Akamine R, Koryudzu K, Tsuchiya A, Sadhu SK, Ahmed F, Itoh M, Okamoto R, Ishibashi M.
J Nat Prod (2017) 80 : 2453 -2461
PubMed 28817274 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.97 6.52
Inhibition 8 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4164399 2 6.52
CHEMBL445086 ASCLEPIN 2 6.52
CHEMBL500585 USCHARIN 2 6.40
CHEMBL4166735 2 6.16
CHEMBL495949 CALOTROPIN 2 6.10
CHEMBL360322 2 5.70
CHEMBL449207 USCHARIDIN 2 5.62
CHEMBL4176111 2 4.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4164399 IC50 = 300.0 nM 6.52
CHEMBL445086 ASCLEPIN IC50 = 300.0 nM 6.52
CHEMBL500585 USCHARIN IC50 = 400.0 nM 6.40
CHEMBL4166735 IC50 = 700.0 nM 6.16
CHEMBL495949 CALOTROPIN IC50 = 800.0 nM 6.10
CHEMBL360322 IC50 = 2000.0 nM 5.70
CHEMBL449207 USCHARIDIN IC50 = 2400.0 nM 5.62
CHEMBL4176111 IC50 = 17300.0 nM 4.76
CHEMBL500585 USCHARIN Inhibition - % -
CHEMBL445086 ASCLEPIN Inhibition - % -
CHEMBL4164399 Inhibition - % -
CHEMBL495949 CALOTROPIN Inhibition - % -
CHEMBL360322 Inhibition - % -
CHEMBL449207 USCHARIDIN Inhibition - % -
CHEMBL4176111 Inhibition - % -
CHEMBL4166735 Inhibition - % -