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Assay Detail

CHEMBL3102209

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

Binding
Inhibition of LPS-induced NF-kappaB activation in mouse RAW264.7 cells treated 30 mins before LPS challenge measured after 6 hrs by luciferase reporter gene assay
25
Total Activities
24
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type RAW264.7
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of novel antitumor dibenzocyclooctatetraene derivatives and related biphenyls as potent inhibitors of NF-κB signaling pathway.
Yu FL, He XY, Gu C, Ohkoshi E, Wang LT, Wang SB, Lai CY, Yu L, Morris-Natschke SL, Lee KH, Liu S, Xie L.
Bioorg Med Chem (2014) 22 : 325 -333
PubMed 24315191 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.84 6.28
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3099444 1 6.28
CHEMBL3099443 2 6.28
CHEMBL475942 1 6.12
CHEMBL3099442 1 6.09
CHEMBL3099434 1 6.05
CHEMBL3099445 1 5.99
CHEMBL3099441 1 5.79
CHEMBL3099452 1 5.79
CHEMBL3099437 1 5.76
CHEMBL403183 1 5.76
CHEMBL3099451 1 5.75
CHEMBL3099438 1 5.67
CHEMBL3099449 1 5.52
CHEMBL3099439 1 5.43
CHEMBL3099440 1 5.38
CHEMBL3099453 1 -
CHEMBL3099454 1 -
CHEMBL3099450 1 -
CHEMBL3099435 1 -
CHEMBL428647 PACLITAXEL 4.0 1 -
CHEMBL3099448 1 -
CHEMBL3099447 1 -
CHEMBL3099446 1 -
CHEMBL3099436 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3099444 IC50 = 520.0 nM 6.28
CHEMBL3099443 IC50 = 520.0 nM 6.28
CHEMBL475942 IC50 = 750.0 nM 6.12
CHEMBL3099442 IC50 = 810.0 nM 6.09
CHEMBL3099434 IC50 = 900.0 nM 6.05
CHEMBL3099445 IC50 = 1020.0 nM 5.99
CHEMBL3099441 IC50 = 1610.0 nM 5.79
CHEMBL3099452 IC50 = 1610.0 nM 5.79
CHEMBL3099437 IC50 = 1720.0 nM 5.76
CHEMBL403183 IC50 = 1720.0 nM 5.76
CHEMBL3099451 IC50 = 1780.0 nM 5.75
CHEMBL3099438 IC50 = 2160.0 nM 5.67
CHEMBL3099449 IC50 = 3020.0 nM 5.52
CHEMBL3099439 IC50 = 3750.0 nM 5.43
CHEMBL3099440 IC50 = 4160.0 nM 5.38
CHEMBL3099453 IC50 - -
CHEMBL3099454 IC50 - -
CHEMBL3099450 IC50 - -
CHEMBL3099435 IC50 - -
CHEMBL428647 PACLITAXEL IC50 - -
CHEMBL3099448 IC50 - -
CHEMBL3099447 IC50 - -
CHEMBL3099446 IC50 - -
CHEMBL3099436 IC50 - -
CHEMBL3099443 Inhibition - % -