Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5055816

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

Functional
Antiinflammatory activity against human THP-1 cells assessed as reduction in LPS and BzATP-induced IL-1beta release measured after 50 mins by microplate reader
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

THP-1 (CHEMBL614245)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139.
Hopper AT, Juhl M, Hornberg J, Badolo L, Kilburn JP, Thougaard A, Smagin G, Song D, Calice L, Menon V, Dale E, Zhang H, Cajina M, Nattini ME, Gandhi A, Grenon M, Jones K, Khayrullina T, Chandrasena G, Thomsen C, Zorn SH, Brodbeck R, Poda SB, Staal R, Möller T.
J Med Chem (2021) 64 : 4891 -4902
PubMed 33822617 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.42 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1628690 1 7.82
CHEMBL3952549 1 7.57
CHEMBL5086274 1 7.42
CHEMBL437703 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1628690 IC50 = 15.0 nM 7.82
CHEMBL3952549 IC50 = 27.0 nM 7.57
CHEMBL5086274 IC50 = 38.0 nM 7.42
CHEMBL437703 IC50 = 140.0 nM 6.85