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Assay Detail

CHEMBL5029686

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

Functional
Down modulation of sortilin expression in HEK293T cells tranfected with GFP-tagged sortilin incubated for 24 hrs by flow cytometric analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK-293T
Confidence 1 — Organism
Curated By Autocuration

Target

HEK-293T (CHEMBL3706568)
Type CELL-LINE
Organism Homo sapiens

Publication

Reduction of Progranulin-Induced Breast Cancer Stem Cell Propagation by Sortilin-Targeting Cyclotriazadisulfonamide (CADA) Compounds.
Berger K, Pauwels E, Parkinson G, Landberg G, Le T, Demillo VG, Lumangtad LA, Jones DE, Islam MA, Olsen R, Kapri T, Intasiri A, Vermeire K, Rhost S, Bell TW.
J Med Chem (2021) 64 : 12865 -12876
PubMed 34428050 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.88 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5089500 1 7.00
CHEMBL1819187 1 6.30
CHEMBL5086848 1 6.00
CHEMBL5092871 1 5.72
CHEMBL1819181 CYCLOTRIAZADISULFONAMIDE HYDROCHLORIDE 1 5.66
CHEMBL4748787 1 5.40
CHEMBL5081066 1 5.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5089500 IC50 = 100.0 nM 7.00
CHEMBL1819187 IC50 = 500.0 nM 6.30
CHEMBL5086848 IC50 = 1000.0 nM 6.00
CHEMBL5092871 IC50 = 1900.0 nM 5.72
CHEMBL1819181 CYCLOTRIAZADISULFONAMIDE HYDROCHLORIDE IC50 = 2200.0 nM 5.66
CHEMBL4748787 IC50 = 4000.0 nM 5.40
CHEMBL5081066 IC50 = 9000.0 nM 5.05