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Assay Detail

CHEMBL1042151

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

Binding
Inhibition of gamma-secretase-mediated cleavage of human APP expressed in CHO cells assessed as reduction in amyloid beta42 production after 24 hrs by double sandwich ELISA
48
Total Activities
48
Compounds Tested
2
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

Synthesis and structure-activity relationship of a novel series of heterocyclic sulfonamide gamma-secretase inhibitors.
Pu J, Kreft AF, Aschmies SH, Atchison KP, Berkowitz J, Caggiano TJ, Chlenov M, Diamantidis G, Harrison BL, Hu Y, Huryn D, Steven Jacobsen J, Jin M, Lipinski K, Lu P, Martone RL, Morris K, Sonnenberg-Reines J, Riddell DR, Sabalski J, Sun SC, Wagner E, Wang Y, Xu Z, Zhou H, Resnick L.
Bioorg Med Chem (2009) 17 : 4708 -4717
PubMed 19443228 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 47 - -
EC50 1 7.54 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL480558 GSI-136 1.0 1 7.54
CHEMBL576531 1 -
CHEMBL577787 1 -
CHEMBL576151 1 -
CHEMBL573631 1 -
CHEMBL576553 1 -
CHEMBL573866 1 -
CHEMBL575640 1 -
CHEMBL575644 1 -
CHEMBL584803 1 -
CHEMBL576136 1 -
CHEMBL572426 1 -
CHEMBL572659 1 -
CHEMBL574537 1 -
CHEMBL574767 1 -
CHEMBL577587 1 -
CHEMBL572436 1 -
CHEMBL573841 1 -
CHEMBL578011 1 -
CHEMBL574531 1 -
CHEMBL576332 1 -
CHEMBL572668 1 -
CHEMBL579055 1 -
CHEMBL575643 1 -
CHEMBL564353 1 -
CHEMBL574309 1 -
CHEMBL572435 1 -
CHEMBL573595 1 -
CHEMBL577579 1 -
CHEMBL574078 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL480558 GSI-136 EC50 = 29.0 nM 7.54
CHEMBL575642 Activity - -
CHEMBL573866 Activity - -
CHEMBL576553 Activity - -
CHEMBL573631 Activity - -
CHEMBL576151 Activity - -
CHEMBL577787 Activity - -
CHEMBL573303 Activity - -
CHEMBL576776 Activity - -
CHEMBL574519 Activity - -
CHEMBL577586 Activity - -
CHEMBL574525 Activity - -
CHEMBL578849 Activity - -
CHEMBL575640 Activity - -
CHEMBL573124 Activity - -
CHEMBL577166 Activity - -
CHEMBL574748 Activity - -
CHEMBL574326 Activity - -
CHEMBL574325 Activity - -
CHEMBL576354 Activity - -
CHEMBL576972 Activity - -
CHEMBL577800 Activity - -
CHEMBL579060 Activity - -
CHEMBL572425 Activity - -
CHEMBL574079 Activity - -
CHEMBL578011 Activity - -
CHEMBL574078 Activity - -
CHEMBL577579 Activity - -
CHEMBL573595 Activity - -
CHEMBL572435 Activity - -
CHEMBL574309 Activity - -
CHEMBL564353 Activity - -
CHEMBL575643 Activity - -
CHEMBL579055 Activity - -
CHEMBL572668 Activity - -
CHEMBL576332 Activity - -
CHEMBL574531 Activity - -
CHEMBL575644 Activity - -
CHEMBL573841 Activity - -
CHEMBL572436 Activity - -
CHEMBL576531 Activity - -
CHEMBL577587 Activity - -
CHEMBL574767 Activity - -
CHEMBL574537 Activity - -
CHEMBL572659 Activity - -
CHEMBL572426 Activity - -
CHEMBL576136 Activity - -
CHEMBL584803 Activity - -