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Assay Detail

CHEMBL2155446

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

Binding
Inhibition of gamma secretase assessed as reduction in Abeta42 production
127
Total Activities
127
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

γ-Secretase modulators as potential disease modifying anti-Alzheimer's drugs.
Oehlrich D, Berthelot DJ, Gijsen HJ.
J Med Chem (2011) 54 : 669 -698
PubMed 21141968 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 127 6.83 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2151221 1 8.70
CHEMBL2151309 1 8.40
CHEMBL2151107 1 8.30
CHEMBL2151219 1 8.30
CHEMBL2151164 1 8.22
CHEMBL2151308 1 8.22
CHEMBL2151306 1 8.10
CHEMBL2151165 1 8.05
CHEMBL2151220 1 8.00
CHEMBL2151159 1 7.96
CHEMBL2151204 1 7.96
CHEMBL2151307 1 7.96
CHEMBL2151116 1 7.92
CHEMBL2151217 1 7.85
CHEMBL2151202 1 7.85
CHEMBL2151200 1 7.85
CHEMBL2151111 1 7.80
CHEMBL2151205 E-2212 1.0 1 7.77
CHEMBL2151113 1 7.75
CHEMBL2151218 1 7.68
CHEMBL2151230 1 7.68
CHEMBL2151203 1 7.66
CHEMBL2151176 1 7.66
CHEMBL2151177 1 7.60
CHEMBL2151198 1 7.55
CHEMBL2151199 1 7.51
CHEMBL2151106 1 7.48
CHEMBL2151115 1 7.48
CHEMBL2151201 1 7.43
CHEMBL2151166 1 7.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2151221 IC50 = 2.0 nM 8.70
CHEMBL2151309 IC50 = 4.0 nM 8.40
CHEMBL2151107 IC50 = 5.0 nM 8.30
CHEMBL2151219 IC50 = 5.0 nM 8.30
CHEMBL2151308 IC50 = 6.0 nM 8.22
CHEMBL2151164 IC50 = 6.0 nM 8.22
CHEMBL2151306 IC50 = 8.0 nM 8.10
CHEMBL2151165 IC50 = 9.0 nM 8.05
CHEMBL2151220 IC50 = 10.0 nM 8.00
CHEMBL2151307 IC50 = 11.0 nM 7.96
CHEMBL2151204 IC50 = 11.0 nM 7.96
CHEMBL2151159 IC50 = 11.0 nM 7.96
CHEMBL2151116 IC50 = 12.0 nM 7.92
CHEMBL2151202 IC50 = 14.0 nM 7.85
CHEMBL2151200 IC50 = 14.0 nM 7.85
CHEMBL2151217 IC50 = 14.0 nM 7.85
CHEMBL2151111 IC50 = 16.0 nM 7.80
CHEMBL2151205 E-2212 IC50 = 17.0 nM 7.77
CHEMBL2151113 IC50 = 18.0 nM 7.75
CHEMBL2151230 IC50 = 21.0 nM 7.68
CHEMBL2151218 IC50 = 21.0 nM 7.68
CHEMBL2151176 IC50 = 22.0 nM 7.66
CHEMBL2151203 IC50 = 22.0 nM 7.66
CHEMBL2151177 IC50 = 25.0 nM 7.60
CHEMBL2151198 IC50 = 28.0 nM 7.55
CHEMBL2151199 IC50 = 31.0 nM 7.51
CHEMBL2151106 IC50 = 33.0 nM 7.48
CHEMBL2151115 IC50 = 33.0 nM 7.48
CHEMBL2151201 IC50 = 37.0 nM 7.43
CHEMBL2151166 IC50 = 39.0 nM 7.41
CHEMBL1915569 IC50 = 40.0 nM 7.40
CHEMBL2151108 IC50 = 41.0 nM 7.39
CHEMBL2151212 IC50 = 44.0 nM 7.36
CHEMBL2151109 IC50 = 60.0 nM 7.22
CHEMBL2151102 IC50 = 60.0 nM 7.22
CHEMBL2151103 IC50 = 60.0 nM 7.22
CHEMBL2151082 IC50 = 65.0 nM 7.19
CHEMBL2151085 IC50 = 69.0 nM 7.16
CHEMBL2151101 IC50 = 70.0 nM 7.16
CHEMBL2151171 IC50 = 70.0 nM 7.16
CHEMBL2151112 IC50 = 76.0 nM 7.12
CHEMBL2151110 IC50 = 76.0 nM 7.12
CHEMBL2151231 IC50 = 80.0 nM 7.10
CHEMBL2151068 IC50 = 80.0 nM 7.10
CHEMBL2151234 IC50 = 83.0 nM 7.08
CHEMBL2151229 IC50 = 84.0 nM 7.08
CHEMBL2151284 IC50 = 90.0 nM 7.05
CHEMBL2151215 IC50 = 101.0 nM 7.00
CHEMBL2151216 IC50 = 101.0 nM 7.00
CHEMBL2151277 IC50 = 100.0 nM 7.00