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Assay Detail

CHEMBL854203

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Binding
Inhibition of gamma secretase
13
Total Activities
13
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

3,4-Fused cyclohexyl sulfones as gamma-secretase inhibitors.
Shaw D, Best J, Dinnell K, Nadin A, Shearman M, Pattison C, Peachey J, Reilly M, Williams B, Wrigley J, Harrison T.
Bioorg Med Chem Lett (2006) 16 : 3073 -3077
PubMed 16617016 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 9.43 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL209888 1 10.40
CHEMBL377691 1 10.22
CHEMBL379089 1 10.10
CHEMBL210587 1 9.72
CHEMBL427397 1 9.62
CHEMBL378502 1 9.59
CHEMBL207353 1 9.40
CHEMBL207454 1 9.39
CHEMBL377264 1 9.12
CHEMBL384207 1 9.05
CHEMBL377367 1 8.93
CHEMBL208089 1 8.86
CHEMBL210279 1 8.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL209888 IC50 = 0.04 nM 10.40
CHEMBL377691 IC50 = 0.06 nM 10.22
CHEMBL379089 IC50 = 0.08 nM 10.10
CHEMBL210587 IC50 = 0.19 nM 9.72
CHEMBL427397 IC50 = 0.24 nM 9.62
CHEMBL378502 IC50 = 0.26 nM 9.59
CHEMBL207353 IC50 = 0.4 nM 9.40
CHEMBL207454 IC50 = 0.41 nM 9.39
CHEMBL377264 IC50 = 0.76 nM 9.12
CHEMBL384207 IC50 = 0.9 nM 9.05
CHEMBL377367 IC50 = 1.17 nM 8.93
CHEMBL208089 IC50 = 1.39 nM 8.86
CHEMBL210279 IC50 = 6.18 nM 8.21