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Assay Detail

CHEMBL4480674

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

Binding
Inhibition of NFkappaB (unknown origin) expressed in human A549 cells co-transfected with pNFkappaB-Luc vector assessed as reduction in TNFalpha-induced NFkappaB transcriptional activity co-incubated for 7 hrs in presence of TNFalpha by bright-glo luciferase reporter gene assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A549
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and discovery of asiatic acid based 1,2,3-triazole derivatives as antitumor agents blocking NF-κB activation and cell migration.
Huang RZ, Liang GB, Li MS, Fang YL, Zhao SF, Zhou MM, Liao ZX, Sun J, Wang HS.
Medchemcomm (2019) 10 : 584 -597
PubMed 31057738 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 5.40 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4527184 1 6.85
CHEMBL4536080 1 6.64
CHEMBL4584388 1 6.04
CHEMBL4546759 1 5.97
CHEMBL536151 IMD-0354 1.0 1 5.90
CHEMBL4569827 1 5.73
CHEMBL4569938 1 5.48
CHEMBL4588898 1 5.32
CHEMBL4574466 1 5.27
CHEMBL4568908 1 5.11
CHEMBL4544481 1 5.09
CHEMBL4540546 1 4.97
CHEMBL4537215 1 4.92
CHEMBL4558718 1 4.88
CHEMBL4589018 1 4.82
CHEMBL4526855 1 4.76
CHEMBL4553112 1 4.72
CHEMBL4592953 1 4.70
CHEMBL4573939 1 -
CHEMBL4548785 1 -
CHEMBL4530301 1 -
CHEMBL404313 ASIATIC ACID 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4527184 IC50 = 140.0 nM 6.85
CHEMBL4536080 IC50 = 230.0 nM 6.64
CHEMBL4584388 IC50 = 920.0 nM 6.04
CHEMBL4546759 IC50 = 1060.0 nM 5.97
CHEMBL536151 IMD-0354 IC50 = 1270.0 nM 5.90
CHEMBL4569827 IC50 = 1880.0 nM 5.73
CHEMBL4569938 IC50 = 3320.0 nM 5.48
CHEMBL4588898 IC50 = 4780.0 nM 5.32
CHEMBL4574466 IC50 = 5390.0 nM 5.27
CHEMBL4568908 IC50 = 7860.0 nM 5.11
CHEMBL4544481 IC50 = 8170.0 nM 5.09
CHEMBL4540546 IC50 = 10610.0 nM 4.97
CHEMBL4537215 IC50 = 12150.0 nM 4.92
CHEMBL4558718 IC50 = 13280.0 nM 4.88
CHEMBL4589018 IC50 = 15040.0 nM 4.82
CHEMBL4526855 IC50 = 17260.0 nM 4.76
CHEMBL4553112 IC50 = 18840.0 nM 4.72
CHEMBL4592953 IC50 = 19790.0 nM 4.70
CHEMBL4573939 IC50 > 20000.0 nM -
CHEMBL4548785 IC50 > 20000.0 nM -
CHEMBL4530301 IC50 > 20000.0 nM -
CHEMBL404313 ASIATIC ACID IC50 > 20000.0 nM -