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Assay Detail

CHEMBL947795

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

Binding
Inhibition of gamma-secretase by Notch-1 cleavage assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

(S)-N-(5-Chlorothiophene-2-sulfonyl)-beta,beta-diethylalaninol a Notch-1-sparing gamma-secretase inhibitor.
Cole DC, Stock JR, Kreft AF, Antane M, Aschmies SH, Atchison KP, Casebier DS, Comery TA, Diamantidis G, Ellingboe JW, Harrison BL, Hu Y, Jin M, Kubrak DM, Lu P, Mann CW, Martone RL, Moore WJ, Oganesian A, Riddell DR, Sonnenberg-Reines J, Sun SC, Wagner E, Wang Z, Woller KR, Xu Z, Zhou H, Jacobsen JS.
Bioorg Med Chem Lett (2009) 19 : 926 -929
PubMed 19097890 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 6.58 6.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL480558 GSI-136 1.0 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL480558 GSI-136 EC50 = 266.0 nM 6.58