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Assay Detail

CHEMBL921620

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Functional
Inhibition of TNF-alpha-stimulated E-selectin promoter transfected human A549 cells after 6 hrs
9
Total Activities
9
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

Synthesis and structure-activity relationship of aminopyrimidine IKK2 inhibitors.
Bingham AH, Davenport RJ, Fosbeary R, Gowers L, Knight RL, Lowe C, Owen DA, Parry DM, Pitt WR.
Bioorg Med Chem Lett (2008) 18 : 3622 -3627
PubMed 18501602 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.65 6.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL257402 1 6.54
CHEMBL402628 1 5.90
CHEMBL256523 1 5.82
CHEMBL257189 1 5.74
CHEMBL256524 1 5.72
CHEMBL401919 1 5.68
CHEMBL403615 1 5.42
CHEMBL257805 1 5.24
CHEMBL402041 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL257402 IC50 = 289.0 nM 6.54
CHEMBL402628 IC50 = 1270.0 nM 5.90
CHEMBL256523 IC50 = 1500.0 nM 5.82
CHEMBL257189 IC50 = 1810.0 nM 5.74
CHEMBL256524 IC50 = 1920.0 nM 5.72
CHEMBL401919 IC50 = 2080.0 nM 5.68
CHEMBL403615 IC50 = 3820.0 nM 5.42
CHEMBL257805 IC50 = 5700.0 nM 5.24
CHEMBL402041 IC50 = 17800.0 nM 4.75