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Assay Detail

CHEMBL4222654

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

Binding
Modulation of human wild-type APP695 expressed in SH-SY5Y cells assessed as inhibition of amyloid beta (1 to 42 residues) production measured after 24 hrs by ELISA
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SH-SY5Y
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Amyloid-beta precursor protein (CHEMBL2487)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New phenylaniline derivatives as modulators of amyloid protein precursor metabolism.
Gay M, Carato P, Coevoet M, Renault N, Larchanché PE, Barczyk A, Yous S, Buée L, Sergeant N, Melnyk P.
Bioorg Med Chem (2018) 26 : 2151 -2164
PubMed 29559198 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 5.24 5.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4226945 1 5.72
CHEMBL319756 1 5.68
CHEMBL317760 1 5.55
CHEMBL97247 1 5.54
CHEMBL4226951 1 5.33
CHEMBL4227472 1 5.31
CHEMBL682 AMODIAQUINE 4.0 1 5.27
CHEMBL4226025 1 5.22
CHEMBL94521 1 5.15
CHEMBL4225563 1 5.10
CHEMBL4228998 1 5.03
CHEMBL138623 1 4.98
CHEMBL167970 1 4.95
CHEMBL76 CHLOROQUINE 4.0 1 4.89
CHEMBL451753 1 4.86
CHEMBL4227963 1 -
CHEMBL4226530 1 -
CHEMBL4227244 1 -
CHEMBL4227708 1 -
CHEMBL4226641 1 -
CHEMBL4226598 1 -
CHEMBL4226906 1 -
CHEMBL4226332 1 -
CHEMBL4226959 1 -
CHEMBL4225842 1 -
CHEMBL4225384 1 -
CHEMBL4226684 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4226945 IC50 = 1900.0 nM 5.72
CHEMBL319756 IC50 = 2100.0 nM 5.68
CHEMBL317760 IC50 = 2800.0 nM 5.55
CHEMBL97247 IC50 = 2900.0 nM 5.54
CHEMBL4226951 IC50 = 4700.0 nM 5.33
CHEMBL4227472 IC50 = 4900.0 nM 5.31
CHEMBL682 AMODIAQUINE IC50 = 5400.0 nM 5.27
CHEMBL4226025 IC50 = 6000.0 nM 5.22
CHEMBL94521 IC50 = 7100.0 nM 5.15
CHEMBL4225563 IC50 = 7900.0 nM 5.10
CHEMBL4228998 IC50 = 9400.0 nM 5.03
CHEMBL138623 IC50 = 10400.0 nM 4.98
CHEMBL167970 IC50 = 11200.0 nM 4.95
CHEMBL76 CHLOROQUINE IC50 = 12800.0 nM 4.89
CHEMBL451753 IC50 = 13800.0 nM 4.86
CHEMBL4227963 IC50 > 10000.0 nM -
CHEMBL4226530 IC50 > 10000.0 nM -
CHEMBL4227244 IC50 > 10000.0 nM -
CHEMBL4227708 IC50 > 10000.0 nM -
CHEMBL4226641 IC50 > 10000.0 nM -
CHEMBL4226598 IC50 > 10000.0 nM -
CHEMBL4226906 IC50 > 10000.0 nM -
CHEMBL4226332 IC50 > 10000.0 nM -
CHEMBL4226959 IC50 > 10000.0 nM -
CHEMBL4225842 IC50 > 10000.0 nM -
CHEMBL4225384 IC50 > 10000.0 nM -
CHEMBL4226684 IC50 > 10000.0 nM -