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Assay Detail

CHEMBL4430528

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

Binding
Inhibition of human NOD2 over-expressed in HEK-Blue cells assessed as inhibition of C12-iE-DAP induced NF-kappaB transcriptional activity preincubated for 1 hr followed by addition of C12-iE-DAP measured after 18 hrs by SEAP reporter gene assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Identification of indole scaffold-based dual inhibitors of NOD1 and NOD2.
Keček Plešec K, Urbančič D, Gobec M, Pekošak A, Tomašič T, Anderluh M, Mlinarič-Raščan I, Jakopin Ž.
Bioorg Med Chem (2016) 24 : 5221 -5234
PubMed 27601373 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.79 5.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4472193 1 5.19
CHEMBL4474194 1 5.04
CHEMBL1314048 1 4.92
CHEMBL4586513 1 4.90
CHEMBL4462798 1 4.77
CHEMBL378112 1 4.63
CHEMBL4534055 1 4.61
CHEMBL1412853 1 4.26
CHEMBL4451566 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4472193 IC50 = 6450.0 nM 5.19
CHEMBL4474194 IC50 = 9040.0 nM 5.04
CHEMBL1314048 IC50 = 11900.0 nM 4.92
CHEMBL4586513 IC50 = 12600.0 nM 4.90
CHEMBL4462798 IC50 = 16900.0 nM 4.77
CHEMBL378112 IC50 = 23400.0 nM 4.63
CHEMBL4534055 IC50 = 24600.0 nM 4.61
CHEMBL1412853 IC50 = 54900.0 nM 4.26
CHEMBL4451566 IC50 > 25000.0 nM -