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Assay Detail

CHEMBL4701727

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

Binding
Modulation of gamma secretase (unknown origin) assessed as inhibition of amyloid beta (1 to 42 residues) production
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Gamma-secretase (CHEMBL2094135)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Synthesis of functionalized derivatives of the gamma-secretase modulator BMS-932481 and identification of its major metabolite.
Zhang Y,Boy KM,Wu YJ,Ramirez A,Toyn JH,Ahlijanian MK,Albright CF,Zhuo X,Johnson BM,Denton RR,Olson RE,Thompson LA,Macor JE
Bioorg Med Chem Lett (2020) 30 : 127530 -127530
PubMed 32890687 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.52 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4209316 1 8.40
CHEMBL4757307 1 8.30
CHEMBL4753645 1 8.00
CHEMBL4757003 1 7.85
CHEMBL4782161 1 7.77
CHEMBL4793756 1 7.50
CHEMBL4780074 1 7.22
CHEMBL4795926 1 7.02
CHEMBL4763646 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4209316 IC50 = 4.0 nM 8.40
CHEMBL4757307 IC50 = 5.0 nM 8.30
CHEMBL4753645 IC50 = 10.0 nM 8.00
CHEMBL4757003 IC50 = 14.0 nM 7.85
CHEMBL4782161 IC50 = 17.0 nM 7.77
CHEMBL4793756 IC50 = 32.0 nM 7.50
CHEMBL4780074 IC50 = 60.0 nM 7.22
CHEMBL4795926 IC50 = 96.0 nM 7.02
CHEMBL4763646 IC50 = 2300.0 nM 5.64