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Assay Detail

CHEMBL946815

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

Binding
Induction of human IkappaBalpha stabilization in OCI-Ly3 cells by green light emiting IkappaBalpha-fused luciferase reporter gene assay
39
Total Activities
39
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type OCI-Ly3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

NF-kappa-B inhibitor alpha (CHEMBL2898)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFkappaB activity within two separate high-throughput screens of NFkappaB activation.
Xie Y, Deng S, Thomas CJ, Liu Y, Zhang YQ, Rinderspacher A, Huang W, Gong G, Wyler M, Cayanis E, Aulner N, Többen U, Chung C, Pampou S, Southall N, Vidović D, Schürer S, Branden L, Davis RE, Staudt LM, Inglese J, Austin CP, Landry DW, Smith DH, Auld DS.
Bioorg Med Chem Lett (2008) 18 : 329 -335
PubMed 18024113 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 38 5.40 6.30
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL271669 1 6.30
CHEMBL272552 1 6.16
CHEMBL64925 MG-132 1 6.00
CHEMBL429586 1 6.00
CHEMBL429599 1 5.96
CHEMBL404128 1 5.89
CHEMBL272553 1 5.89
CHEMBL273149 1 5.85
CHEMBL256403 1 5.85
CHEMBL428064 1 5.66
CHEMBL257446 1 5.57
CHEMBL404588 1 5.44
CHEMBL273147 1 5.43
CHEMBL256061 1 5.40
CHEMBL270799 1 5.39
CHEMBL257234 1 5.28
CHEMBL401504 1 5.23
CHEMBL402638 1 5.22
CHEMBL256609 1 5.21
CHEMBL540966 1 5.19
CHEMBL256204 1 5.17
CHEMBL269942 1 5.17
CHEMBL256042 1 5.17
CHEMBL270798 1 5.16
CHEMBL258314 1 5.10
CHEMBL403333 1 5.10
CHEMBL273148 1 5.05
CHEMBL401505 1 5.03
CHEMBL269941 1 5.00
CHEMBL256062 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL271669 EC50 = 500.0 nM 6.30
CHEMBL272552 EC50 = 700.0 nM 6.16
CHEMBL429586 EC50 = 1000.0 nM 6.00
CHEMBL64925 MG-132 EC50 = 1000.0 nM 6.00
CHEMBL429599 EC50 = 1100.0 nM 5.96
CHEMBL404128 EC50 = 1300.0 nM 5.89
CHEMBL272553 EC50 = 1300.0 nM 5.89
CHEMBL273149 EC50 = 1400.0 nM 5.85
CHEMBL256403 EC50 = 1400.0 nM 5.85
CHEMBL428064 EC50 = 2200.0 nM 5.66
CHEMBL257446 EC50 = 2700.0 nM 5.57
CHEMBL404588 EC50 = 3600.0 nM 5.44
CHEMBL273147 EC50 = 3700.0 nM 5.43
CHEMBL256061 EC50 = 4000.0 nM 5.40
CHEMBL270799 EC50 = 4100.0 nM 5.39
CHEMBL257234 EC50 = 5300.0 nM 5.28
CHEMBL401504 EC50 = 5900.0 nM 5.23
CHEMBL402638 EC50 = 6000.0 nM 5.22
CHEMBL256609 EC50 = 6100.0 nM 5.21
CHEMBL540966 EC50 = 6500.0 nM 5.19
CHEMBL269942 EC50 = 6800.0 nM 5.17
CHEMBL256042 EC50 = 6800.0 nM 5.17
CHEMBL256204 EC50 = 6800.0 nM 5.17
CHEMBL270798 EC50 = 7000.0 nM 5.16
CHEMBL258314 EC50 = 8000.0 nM 5.10
CHEMBL403333 EC50 = 8000.0 nM 5.10
CHEMBL273148 EC50 = 8900.0 nM 5.05
CHEMBL401505 EC50 = 9400.0 nM 5.03
CHEMBL269941 EC50 = 10000.0 nM 5.00
CHEMBL256062 EC50 = 11000.0 nM 4.96
CHEMBL270605 EC50 = 11000.0 nM 4.96
CHEMBL257286 EC50 = 17000.0 nM 4.77
CHEMBL256244 EC50 = 20000.0 nM 4.70
CHEMBL129857 AS-602868 Activity - -
CHEMBL271233 EC50 - -
CHEMBL403922 EC50 > 20000.0 nM -
CHEMBL256243 EC50 > 10000.0 nM -
CHEMBL270584 EC50 - -
CHEMBL255537 EC50 - -