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Assay Detail

CHEMBL1177264

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

Binding
Modulation of gamma-secretase-mediated cleavage of human APP expressed in CHO cells with human presenilin-1 assessed as activation of amyloid beta38 production after 24 hrs by ELISA
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design, synthesis, and biological evaluation of a novel class of gamma-secretase modulators with PPARgamma activity.
Hieke M, Ness J, Steri R, Dittrich M, Greiner C, Werz O, Baumann K, Schubert-Zsilavecz M, Weggen S, Zettl H.
J Med Chem (2010) 53 : 4691 -4700
PubMed 20503989 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 5.00 5.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1170264 1 5.75
CHEMBL1171833 1 5.72
CHEMBL1171834 1 5.34
CHEMBL1170852 1 5.26
CHEMBL1173121 1 5.21
CHEMBL1173376 1 5.19
CHEMBL1173564 1 5.08
CHEMBL1172000 1 5.05
CHEMBL1172002 1 4.96
CHEMBL461883 1 4.95
CHEMBL1171851 1 4.89
CHEMBL1170076 1 4.87
CHEMBL1172016 1 4.79
CHEMBL1172019 1 4.79
CHEMBL1171832 1 4.76
CHEMBL1172222 1 4.62
CHEMBL1172003 1 4.62
CHEMBL1172001 1 4.62
CHEMBL1173499 1 4.51
CHEMBL1171652 1 -
CHEMBL1171831 1 -
CHEMBL518507 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1170264 EC50 = 1800.0 nM 5.75
CHEMBL1171833 EC50 = 1900.0 nM 5.72
CHEMBL1171834 EC50 = 4600.0 nM 5.34
CHEMBL1170852 EC50 = 5500.0 nM 5.26
CHEMBL1173121 EC50 = 6200.0 nM 5.21
CHEMBL1173376 EC50 = 6400.0 nM 5.19
CHEMBL1173564 EC50 = 8400.0 nM 5.08
CHEMBL1172000 EC50 = 9000.0 nM 5.05
CHEMBL1172002 EC50 = 10900.0 nM 4.96
CHEMBL461883 EC50 = 11300.0 nM 4.95
CHEMBL1171851 EC50 = 12800.0 nM 4.89
CHEMBL1170076 EC50 = 13500.0 nM 4.87
CHEMBL1172016 EC50 = 16400.0 nM 4.79
CHEMBL1172019 EC50 = 16400.0 nM 4.79
CHEMBL1171832 EC50 = 17500.0 nM 4.76
CHEMBL1172222 EC50 = 24200.0 nM 4.62
CHEMBL1172003 EC50 = 24200.0 nM 4.62
CHEMBL1172001 EC50 = 24000.0 nM 4.62
CHEMBL1173499 EC50 = 31100.0 nM 4.51
CHEMBL1171652 EC50 - -
CHEMBL1171831 EC50 - -
CHEMBL518507 EC50 > 40000.0 nM -