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Assay Detail

CHEMBL4767807

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

Binding
Antagonist activity at human NOD2 expressed in HEK293 cells assessed as reduction in MDP-induced NF-kappaB activation preincubated for 1 hr followed by MDP stimulation and measured after 18 hrs by SEAP reporter gene based spectrophotometric analysis
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Structural features and functional activities of benzimidazoles as NOD2 antagonists.
Guzelj S,Gobec M,Urbančič D,Mlinarič-Raščan I,Corsini E,Jakopin Ž
Eur J Med Chem (2020) 190 : 112089 -112089
PubMed 32014680 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.10 6.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4778195 1 6.20
CHEMBL4795343 1 5.32
CHEMBL4795701 1 5.29
CHEMBL4792847 1 5.29
CHEMBL4792350 1 5.28
CHEMBL4793309 1 5.24
CHEMBL3321852 1 5.21
CHEMBL4791327 1 5.21
CHEMBL4778560 1 5.06
CHEMBL4795393 1 4.97
CHEMBL4778513 1 4.79
CHEMBL4800550 1 4.64
CHEMBL4781211 1 4.59
CHEMBL1412853 1 4.26
CHEMBL4793456 1 -
CHEMBL4784164 1 -
CHEMBL4793193 1 -
CHEMBL4794455 1 -
CHEMBL4792755 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4778195 IC50 = 630.0 nM 6.20
CHEMBL4795343 IC50 = 4760.0 nM 5.32
CHEMBL4795701 IC50 = 5080.0 nM 5.29
CHEMBL4792847 IC50 = 5120.0 nM 5.29
CHEMBL4792350 IC50 = 5230.0 nM 5.28
CHEMBL4793309 IC50 = 5700.0 nM 5.24
CHEMBL3321852 IC50 = 6200.0 nM 5.21
CHEMBL4791327 IC50 = 6200.0 nM 5.21
CHEMBL4778560 IC50 = 8800.0 nM 5.06
CHEMBL4795393 IC50 = 10600.0 nM 4.97
CHEMBL4778513 IC50 = 16400.0 nM 4.79
CHEMBL4800550 IC50 = 22900.0 nM 4.64
CHEMBL4781211 IC50 = 25900.0 nM 4.59
CHEMBL1412853 IC50 = 54900.0 nM 4.26
CHEMBL4793456 IC50 - -
CHEMBL4784164 IC50 - -
CHEMBL4793193 IC50 - -
CHEMBL4794455 IC50 > 20000.0 nM -
CHEMBL4792755 IC50 - -