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Assay Detail

CHEMBL945015

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

Functional
Inhibition of LPS-stimulated TNFalpha release in human whole blood
28
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Blood
Confidence 1 — Organism
Curated By Autocuration

Target

Blood (CHEMBL613416)
Type TISSUE
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of 8-biarylquinolines: a novel class of PDE4 inhibitors.
Gallant M, Chauret N, Claveau D, Day S, Deschênes D, Dubé D, Huang Z, Lacombe P, Laliberté F, Lévesque JF, Liu S, Macdonald D, Mancini J, Masson P, Mastracchio A, Nicholson D, Nicoll-Griffith DA, Perrier H, Salem M, Styhler A, Young RN, Girard Y.
Bioorg Med Chem Lett (2008) 18 : 1407 -1412
PubMed 18207397 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 6.25 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL252490 1 7.10
CHEMBL251882 1 6.92
CHEMBL252491 1 6.92
CHEMBL252089 1 6.82
CHEMBL372575 1 6.80
CHEMBL252687 1 6.62
CHEMBL252469 1 6.51
CHEMBL254518 1 6.50
CHEMBL252887 1 6.48
CHEMBL403065 1 6.40
CHEMBL403546 1 6.37
CHEMBL252090 1 6.32
CHEMBL436847 1 6.32
CHEMBL403977 1 6.28
CHEMBL252287 1 6.25
CHEMBL251883 1 6.24
CHEMBL402953 1 6.22
CHEMBL253083 2 6.22
CHEMBL401663 1 6.16
CHEMBL252685 1 6.09
CHEMBL252686 1 6.07
CHEMBL252886 1 6.04
CHEMBL253082 1 6.03
CHEMBL252088 1 5.96
CHEMBL403744 1 5.75
CHEMBL252489 1 5.20
CHEMBL252885 1 4.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL252490 IC50 = 80.0 nM 7.10
CHEMBL252491 IC50 = 120.0 nM 6.92
CHEMBL251882 IC50 = 120.0 nM 6.92
CHEMBL252089 IC50 = 150.0 nM 6.82
CHEMBL372575 IC50 = 160.0 nM 6.80
CHEMBL252687 IC50 = 240.0 nM 6.62
CHEMBL252469 IC50 = 310.0 nM 6.51
CHEMBL254518 IC50 = 320.0 nM 6.50
CHEMBL252887 IC50 = 330.0 nM 6.48
CHEMBL403065 IC50 = 400.0 nM 6.40
CHEMBL403546 IC50 = 430.0 nM 6.37
CHEMBL436847 IC50 = 480.0 nM 6.32
CHEMBL252090 IC50 = 480.0 nM 6.32
CHEMBL403977 IC50 = 520.0 nM 6.28
CHEMBL252287 IC50 = 560.0 nM 6.25
CHEMBL251883 IC50 = 580.0 nM 6.24
CHEMBL253083 IC50 = 600.0 nM 6.22
CHEMBL402953 IC50 = 600.0 nM 6.22
CHEMBL401663 IC50 = 700.0 nM 6.16
CHEMBL252685 IC50 = 820.0 nM 6.09
CHEMBL252686 IC50 = 850.0 nM 6.07
CHEMBL252886 IC50 = 920.0 nM 6.04
CHEMBL253082 IC50 = 930.0 nM 6.03
CHEMBL252088 IC50 = 1100.0 nM 5.96
CHEMBL253083 IC50 = 1400.0 nM 5.85
CHEMBL403744 IC50 = 1800.0 nM 5.75
CHEMBL252489 IC50 = 6300.0 nM 5.20
CHEMBL252885 IC50 = 25000.0 nM 4.60