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Assay Detail

CHEMBL945844

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Binding
Inhibition of TNFalpha stimulated human NF-kappaB-mediated beta lactamase gene expression in HUVEC
ChEMBL ↗
40
Total Activities
40
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

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
IC50 39 5.53 6.22
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64925 MG-132 — 1 6.22
CHEMBL271669 — — 1 6.10
CHEMBL257446 — — 1 6.00
CHEMBL402638 — — 1 6.00
CHEMBL273149 — — 1 5.96
CHEMBL272552 — — 1 5.92
CHEMBL256403 — — 1 5.89
CHEMBL404588 — — 1 5.89
CHEMBL404128 — — 1 5.89
CHEMBL429586 — — 1 5.75
CHEMBL270799 — — 1 5.75
CHEMBL429599 — — 1 5.72
CHEMBL272553 — — 1 5.70
CHEMBL129857 AS-602868 1.0 1 5.70
CHEMBL256061 — — 1 5.70
CHEMBL273147 — — 1 5.50
CHEMBL428064 — — 1 5.47
CHEMBL401504 — — 1 5.47
CHEMBL273148 — — 1 5.44
CHEMBL269942 — — 1 5.40
CHEMBL256609 — — 1 5.30
CHEMBL540966 — — 1 5.30
CHEMBL258314 — — 1 5.26
CHEMBL256204 — — 1 5.22
CHEMBL256042 — — 1 5.22
CHEMBL403333 — — 1 5.17
CHEMBL257234 — — 1 5.16
CHEMBL257286 — — 1 5.10
CHEMBL270798 — — 1 5.09
CHEMBL270605 — — 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64925 MG-132 IC50 = 600.0 nM 6.22
CHEMBL271669 — IC50 = 800.0 nM 6.10
CHEMBL402638 — IC50 = 1000.0 nM 6.00
CHEMBL257446 — IC50 = 1000.0 nM 6.00
CHEMBL273149 — IC50 = 1100.0 nM 5.96
CHEMBL272552 — IC50 = 1200.0 nM 5.92
CHEMBL256403 — IC50 = 1300.0 nM 5.89
CHEMBL404588 — IC50 = 1300.0 nM 5.89
CHEMBL404128 — IC50 = 1300.0 nM 5.89
CHEMBL429586 — IC50 = 1800.0 nM 5.75
CHEMBL270799 — IC50 = 1800.0 nM 5.75
CHEMBL429599 — IC50 = 1900.0 nM 5.72
CHEMBL272553 — IC50 = 2000.0 nM 5.70
CHEMBL129857 AS-602868 IC50 = 2000.0 nM 5.70
CHEMBL256061 — IC50 = 2000.0 nM 5.70
CHEMBL273147 — IC50 = 3200.0 nM 5.50
CHEMBL428064 — IC50 = 3400.0 nM 5.47
CHEMBL401504 — IC50 = 3400.0 nM 5.47
CHEMBL273148 — IC50 = 3600.0 nM 5.44
CHEMBL269942 — IC50 = 4000.0 nM 5.40
CHEMBL256609 — IC50 = 5000.0 nM 5.30
CHEMBL540966 — IC50 = 5000.0 nM 5.30
CHEMBL258314 — IC50 = 5500.0 nM 5.26
CHEMBL256204 — IC50 = 6000.0 nM 5.22
CHEMBL256042 — IC50 = 6000.0 nM 5.22
CHEMBL403333 — IC50 = 6700.0 nM 5.17
CHEMBL257234 — IC50 = 7000.0 nM 5.16
CHEMBL257286 — IC50 = 8000.0 nM 5.10
CHEMBL270798 — IC50 = 8100.0 nM 5.09
CHEMBL270605 — IC50 = 10000.0 nM 5.00
CHEMBL269941 — IC50 = 13000.0 nM 4.89
CHEMBL256062 — IC50 = 13500.0 nM 4.87
CHEMBL403183 — IC50 - — -
CHEMBL271233 — IC50 - — -
CHEMBL403922 — IC50 > 57000.0 nM -
CHEMBL256243 — Activity - — -
CHEMBL256244 — IC50 > 57000.0 nM -
CHEMBL401505 — IC50 > 57000.0 nM -
CHEMBL255537 — IC50 - — -
CHEMBL270584 — IC50 - — -