Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1042152

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 beta40 production after 24 hrs by double sandwich ELISA
ChEMBL ↗
48
Total Activities
48
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

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
EC50 48 5.70 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL480558 GSI-136 1.0 1 7.54
CHEMBL576553 — — 1 7.04
CHEMBL576151 — — 1 6.96
CHEMBL575644 — — 1 6.89
CHEMBL574079 — — 1 6.85
CHEMBL578849 — — 1 6.50
CHEMBL575643 — — 1 6.39
CHEMBL574309 — — 1 6.38
CHEMBL576776 — — 1 6.33
CHEMBL577166 — — 1 6.32
CHEMBL577586 — — 1 6.26
CHEMBL572425 — — 1 6.20
CHEMBL574326 — — 1 6.06
CHEMBL579055 — — 1 6.03
CHEMBL576354 — — 1 6.03
CHEMBL574519 — — 1 6.00
CHEMBL574525 — — 1 6.00
CHEMBL574325 — — 1 6.00
CHEMBL574748 — — 1 6.00
CHEMBL584803 — — 1 6.00
CHEMBL564353 — — 1 5.95
CHEMBL572668 — — 1 5.92
CHEMBL573841 — — 1 5.82
CHEMBL577579 — — 1 5.81
CHEMBL572426 — — 1 5.79
CHEMBL576136 — — 1 5.78
CHEMBL572659 — — 1 5.70
CHEMBL574078 — — 1 5.66
CHEMBL574537 — — 1 5.64
CHEMBL572435 — — 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL480558 GSI-136 EC50 = 29.0 nM 7.54
CHEMBL576553 — EC50 = 92.0 nM 7.04
CHEMBL576151 — EC50 = 110.0 nM 6.96
CHEMBL575644 — EC50 = 130.0 nM 6.89
CHEMBL574079 — EC50 = 140.0 nM 6.85
CHEMBL578849 — EC50 = 320.0 nM 6.50
CHEMBL575643 — EC50 = 410.0 nM 6.39
CHEMBL574309 — EC50 = 420.0 nM 6.38
CHEMBL576776 — EC50 = 470.0 nM 6.33
CHEMBL577166 — EC50 = 480.0 nM 6.32
CHEMBL577586 — EC50 = 550.0 nM 6.26
CHEMBL572425 — EC50 = 630.0 nM 6.20
CHEMBL574326 — EC50 = 880.0 nM 6.06
CHEMBL579055 — EC50 = 930.0 nM 6.03
CHEMBL576354 — EC50 = 940.0 nM 6.03
CHEMBL574519 — EC50 = 990.0 nM 6.00
CHEMBL584803 — EC50 = 1000.0 nM 6.00
CHEMBL574748 — EC50 = 990.0 nM 6.00
CHEMBL574325 — EC50 = 1010.0 nM 6.00
CHEMBL574525 — EC50 = 1010.0 nM 6.00
CHEMBL564353 — EC50 = 1120.0 nM 5.95
CHEMBL572668 — EC50 = 1200.0 nM 5.92
CHEMBL573841 — EC50 = 1530.0 nM 5.82
CHEMBL577579 — EC50 = 1560.0 nM 5.81
CHEMBL572426 — EC50 = 1620.0 nM 5.79
CHEMBL576136 — EC50 = 1680.0 nM 5.78
CHEMBL572659 — EC50 = 1980.0 nM 5.70
CHEMBL574078 — EC50 = 2190.0 nM 5.66
CHEMBL574537 — EC50 = 2270.0 nM 5.64
CHEMBL572435 — EC50 = 2530.0 nM 5.60
CHEMBL573595 — EC50 = 2760.0 nM 5.56
CHEMBL575640 — EC50 = 2890.0 nM 5.54
CHEMBL573124 — EC50 = 3360.0 nM 5.47
CHEMBL573866 — EC50 = 8500.0 nM 5.07
CHEMBL576972 — EC50 = 13320.0 nM 4.88
CHEMBL578011 — EC50 = 13360.0 nM 4.87
CHEMBL575642 — EC50 = 19490.0 nM 4.71
CHEMBL577800 — EC50 = 19400.0 nM 4.71
CHEMBL574767 — EC50 = 22970.0 nM 4.64
CHEMBL576531 — EC50 = 25510.0 nM 4.59
CHEMBL572436 — EC50 = 42360.0 nM 4.37
CHEMBL579060 — EC50 = 50630.0 nM 4.30
CHEMBL576332 — EC50 = 65120.0 nM 4.19
CHEMBL574531 — EC50 = 70150.0 nM 4.15
CHEMBL577587 — EC50 = 85240.0 nM 4.07
CHEMBL573303 — EC50 > 15000.0 nM -
CHEMBL577787 — EC50 > 15000.0 nM -
CHEMBL573631 — EC50 > 15000.0 nM -