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Assay Detail

CHEMBL1772418

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

Binding
Effect on gamma secretase-mediated notch processing in C57BL/6 mouse fetal thymic organ cultures assessed as reduction of B and T-cell populations after 45 mins by FACS analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design, synthesis, and in vivo characterization of a novel series of tetralin amino imidazoles as γ-secretase inhibitors: discovery of PF-3084014.
Brodney MA, Auperin DD, Becker SL, Bronk BS, Brown TM, Coffman KJ, Finley JE, Hicks CD, Karmilowicz MJ, Lanz TA, Liston D, Liu X, Martin BA, Nelson RB, Nolan CE, Oborski CE, Parker CP, Richter KE, Pozdnyakov N, Sahagan BG, Schachter JB, Sokolowski SA, Tate B, Wood DE, Wood KM, Van Deusen JW, Zhang L.
Bioorg Med Chem Lett (2011) 21 : 2637 -2640
PubMed 21269827 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 5.54 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1770915 1 5.96
CHEMBL1770916 NIROGACESTAT 4.0 1 5.74
CHEMBL1770912 1 5.59
CHEMBL1770914 1 5.52
CHEMBL1770911 1 5.49
CHEMBL1770917 1 5.29
CHEMBL1770913 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1770915 EC50 = 1090.0 nM 5.96
CHEMBL1770916 NIROGACESTAT EC50 = 1830.0 nM 5.74
CHEMBL1770912 EC50 = 2560.0 nM 5.59
CHEMBL1770914 EC50 = 3010.0 nM 5.52
CHEMBL1770911 EC50 = 3260.0 nM 5.49
CHEMBL1770917 EC50 = 5100.0 nM 5.29
CHEMBL1770913 EC50 = 6100.0 nM 5.21