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Assay Detail

CHEMBL1821160

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

Binding
Modulation of gamma-secretase expressed in CHO cells co-expressing human APP and wild type human presenilin-1 assessed as inhibition of amyloid beta42 production by ELISA
21
Total Activities
21
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

SAR studies of acidic dual γ-secretase/PPARγ modulators.
Hieke M, Ness J, Steri R, Greiner C, Werz O, Schubert-Zsilavecz M, Weggen S, Zettl H.
Bioorg Med Chem (2011) 19 : 5372 -5382
PubMed 21873070 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 4.81 5.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1819479 1 5.92
CHEMBL1819478 1 5.62
CHEMBL1819480 1 5.57
CHEMBL1819398 1 5.41
CHEMBL1170264 1 5.29
CHEMBL1171834 1 5.22
CHEMBL1819397 1 4.81
CHEMBL461883 1 4.64
CHEMBL6 INDOMETHACIN 4.0 1 4.60
CHEMBL1819392 1 4.49
CHEMBL1817687 1 4.47
CHEMBL1819390 1 4.42
CHEMBL1819391 1 4.42
CHEMBL1819393 1 4.10
CHEMBL1819396 1 4.01
CHEMBL1819394 1 4.00
CHEMBL521 IBUPROFEN 4.0 1 -
CHEMBL1316 CARPROFEN 4.0 1 -
CHEMBL1819481 1 -
CHEMBL1819482 1 -
CHEMBL1819483 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1819479 IC50 = 1200.0 nM 5.92
CHEMBL1819478 IC50 = 2400.0 nM 5.62
CHEMBL1819480 IC50 = 2700.0 nM 5.57
CHEMBL1819398 IC50 = 3900.0 nM 5.41
CHEMBL1170264 IC50 = 5100.0 nM 5.29
CHEMBL1171834 IC50 = 6000.0 nM 5.22
CHEMBL1819397 IC50 = 15400.0 nM 4.81
CHEMBL461883 IC50 = 22800.0 nM 4.64
CHEMBL6 INDOMETHACIN IC50 = 25000.0 nM 4.60
CHEMBL1819392 IC50 = 32700.0 nM 4.49
CHEMBL1817687 IC50 = 33700.0 nM 4.47
CHEMBL1819390 IC50 = 38400.0 nM 4.42
CHEMBL1819391 IC50 = 37900.0 nM 4.42
CHEMBL1819393 IC50 = 79000.0 nM 4.10
CHEMBL1819396 IC50 = 97000.0 nM 4.01
CHEMBL1819394 IC50 = 100000.0 nM 4.00
CHEMBL521 IBUPROFEN IC50 = 200000.0 nM -
CHEMBL1316 CARPROFEN IC50 = 305000.0 nM -
CHEMBL1819481 IC50 > 40000.0 nM -
CHEMBL1819482 IC50 > 40000.0 nM -
CHEMBL1819483 IC50 > 40000.0 nM -