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Assay Detail

CHEMBL1177263

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 inhibition of amyloid beta42 production after 24 hrs by ELISA
27
Total Activities
27
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
IC50 27 4.69 5.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1171834 1 5.29
CHEMBL1170264 1 5.22
CHEMBL1170852 1 5.07
CHEMBL1171833 1 4.95
CHEMBL1173376 1 4.89
CHEMBL1172000 1 4.76
CHEMBL1173121 1 4.71
CHEMBL1173564 1 4.67
CHEMBL461883 1 4.64
CHEMBL1172016 1 4.64
CHEMBL1172222 1 4.60
CHEMBL6 INDOMETHACIN 4.0 1 4.60
CHEMBL1172002 1 4.55
CHEMBL1171851 1 4.53
CHEMBL1172003 1 4.52
CHEMBL1172019 1 4.51
CHEMBL1171652 1 4.51
CHEMBL1170076 1 4.49
CHEMBL18797 SULINDAC SULFIDE -1.0 1 4.47
CHEMBL1171832 1 4.42
CHEMBL1173499 1 4.38
CHEMBL521 IBUPROFEN 4.0 1 -
CHEMBL1171831 1 -
CHEMBL518507 1 -
CHEMBL1316 CARPROFEN 4.0 1 -
CHEMBL1172001 1 -
CHEMBL190083 TARENFLURBIL 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1171834 IC50 = 5100.0 nM 5.29
CHEMBL1170264 IC50 = 6000.0 nM 5.22
CHEMBL1170852 IC50 = 8600.0 nM 5.07
CHEMBL1171833 IC50 = 11300.0 nM 4.95
CHEMBL1173376 IC50 = 13000.0 nM 4.89
CHEMBL1172000 IC50 = 17200.0 nM 4.76
CHEMBL1173121 IC50 = 19300.0 nM 4.71
CHEMBL1173564 IC50 = 21500.0 nM 4.67
CHEMBL461883 IC50 = 22800.0 nM 4.64
CHEMBL1172016 IC50 = 22900.0 nM 4.64
CHEMBL1172222 IC50 = 25200.0 nM 4.60
CHEMBL6 INDOMETHACIN IC50 = 25000.0 nM 4.60
CHEMBL1172002 IC50 = 28200.0 nM 4.55
CHEMBL1171851 IC50 = 29300.0 nM 4.53
CHEMBL1172003 IC50 = 30400.0 nM 4.52
CHEMBL1172019 IC50 = 30900.0 nM 4.51
CHEMBL1171652 IC50 = 31200.0 nM 4.51
CHEMBL1170076 IC50 = 32600.0 nM 4.49
CHEMBL18797 SULINDAC SULFIDE IC50 = 34000.0 nM 4.47
CHEMBL1171832 IC50 = 37700.0 nM 4.42
CHEMBL1173499 IC50 = 41600.0 nM 4.38
CHEMBL521 IBUPROFEN IC50 = 200000.0 nM -
CHEMBL1171831 IC50 > 40000.0 nM -
CHEMBL518507 IC50 > 40000.0 nM -
CHEMBL1316 CARPROFEN IC50 = 305000.0 nM -
CHEMBL1172001 IC50 > 40000.0 nM -
CHEMBL190083 TARENFLURBIL IC50 = 305000.0 nM -