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Assay Detail

CHEMBL960918

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

Functional
Inhibition of LPS-induced TNFalpha production in human PBMC preincubated for 30 mins before LPS challenge measured afterr 6 hrs by ELISA
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type PBMC
Confidence 1 — Organism
Curated By Autocuration

Target

PBMC (CHEMBL613107)
Type CELL-LINE
Organism Homo sapiens

Publication

Novel tricyclic inhibitors of IkappaB kinase.
Kempson J, Spergel SH, Guo J, Quesnelle C, Gill P, Belanger D, Dyckman AJ, Li T, Watterson SH, Langevine CM, Das J, Moquin RV, Furch JA, Marinier A, Dodier M, Martel A, Nirschl D, Van Kirk K, Burke JR, Pattoli MA, Gillooly K, McIntyre KW, Chen L, Yang Z, Marathe PH, Wang-Iverson D, Dodd JH, McKinnon M, Barrish JC, Pitts WJ.
J Med Chem (2009) 52 : 1994 -2005
PubMed 19267461 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.23 7.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL522014 1 7.09
CHEMBL493974 1 6.80
CHEMBL494162 1 6.77
CHEMBL521643 1 6.51
CHEMBL454973 1 6.46
CHEMBL493940 1 6.41
CHEMBL522011 1 6.36
CHEMBL522318 1 6.35
CHEMBL493745 1 6.33
CHEMBL505943 1 6.24
CHEMBL492755 1 6.20
CHEMBL492332 1 6.18
CHEMBL492331 1 6.07
CHEMBL504727 1 6.01
CHEMBL492527 1 5.77
CHEMBL454470 1 5.58
CHEMBL447603 1 5.48
CHEMBL523002 1 5.46
CHEMBL492754 1 -
CHEMBL494154 1 -
CHEMBL494153 1 -
CHEMBL506895 1 -
CHEMBL522171 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL522014 IC50 = 82.0 nM 7.09
CHEMBL493974 IC50 = 160.0 nM 6.80
CHEMBL494162 IC50 = 170.0 nM 6.77
CHEMBL521643 IC50 = 310.0 nM 6.51
CHEMBL454973 IC50 = 350.0 nM 6.46
CHEMBL493940 IC50 = 390.0 nM 6.41
CHEMBL522011 IC50 = 440.0 nM 6.36
CHEMBL522318 IC50 = 450.0 nM 6.35
CHEMBL493745 IC50 = 470.0 nM 6.33
CHEMBL505943 IC50 = 580.0 nM 6.24
CHEMBL492755 IC50 = 630.0 nM 6.20
CHEMBL492332 IC50 = 660.0 nM 6.18
CHEMBL492331 IC50 = 850.0 nM 6.07
CHEMBL504727 IC50 = 970.0 nM 6.01
CHEMBL492527 IC50 = 1700.0 nM 5.77
CHEMBL454470 IC50 = 2600.0 nM 5.58
CHEMBL447603 IC50 = 3300.0 nM 5.48
CHEMBL523002 IC50 = 3500.0 nM 5.46
CHEMBL492754 IC50 - -
CHEMBL494154 IC50 - -
CHEMBL494153 IC50 - -
CHEMBL506895 IC50 - -
CHEMBL522171 IC50 - -