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Assay Detail

CHEMBL983957

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

Functional
Inhibition of TNF-alpha-induced NF-kappaB receptor activation in human A549 cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A549
Confidence 1 — Organism
Curated By Autocuration

Target

A549 (CHEMBL392)
Type CELL-LINE
Organism Homo sapiens

Publication

4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors.
Liddle J, Bamborough P, Barker MD, Campos S, Cousins RP, Cutler GJ, Hobbs H, Holmes DS, Ioannou C, Mellor GW, Morse MA, Payne JJ, Pritchard JM, Smith KJ, Tape DT, Whitworth C, Williamson RA.
Bioorg Med Chem Lett (2009) 19 : 2504 -2508
PubMed 19349179 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.15 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL483165 1 7.30
CHEMBL482747 1 6.50
CHEMBL483557 1 6.30
CHEMBL483166 1 6.30
CHEMBL473080 1 6.20
CHEMBL520308 1 6.10
CHEMBL485145 1 6.00
CHEMBL520473 1 5.70
CHEMBL484966 1 5.70
CHEMBL519965 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL483165 IC50 = 50.12 nM 7.30
CHEMBL482747 IC50 = 316.23 nM 6.50
CHEMBL483557 IC50 = 501.19 nM 6.30
CHEMBL483166 IC50 = 501.19 nM 6.30
CHEMBL473080 IC50 = 630.96 nM 6.20
CHEMBL520308 IC50 = 794.33 nM 6.10
CHEMBL485145 IC50 = 1000.0 nM 6.00
CHEMBL520473 IC50 = 1995.26 nM 5.70
CHEMBL484966 IC50 = 1995.26 nM 5.70
CHEMBL519965 IC50 = 3981.07 nM 5.40