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Assay Detail

CHEMBL4700758

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

Functional
Inhibition of amyloid beta (1 to 42) secretion in human H4 cells overexpressing APP incubated for overnight by HTRF analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type H4
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Identification and Preclinical Evaluation of the Bicyclic Pyrimidine γ-Secretase Modulator BMS-932481.
Boy KM,Guernon JM,Zuev DS,Xu L,Zhang Y,Shi J,Marcin LR,Higgins MA,Wu YJ,Krishnananthan S,Li J,Trehan A,Smith D,Toyn JH,Meredith JE,Burton CR,Kimura SR,Zvyaga T,Zhuo X,Lentz KA,Grace JE,Denton R,Morrison JS,Mathur A,Albright CF,Ahlijanian MK,Olson RE,Thompson LA,Macor JE
ACS Med Chem Lett (2019) 10 : 312 -317
PubMed 30891132 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.83 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4794465 1 8.70
CHEMBL4209316 1 8.18
CHEMBL3769487 1 7.51
CHEMBL3769431 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4794465 IC50 = 2.0 nM 8.70
CHEMBL4209316 IC50 = 6.6 nM 8.18
CHEMBL3769487 IC50 = 31.0 nM 7.51
CHEMBL3769431 IC50 = 120.0 nM 6.92