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Assay Detail

CHEMBL1071779

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

Functional
Antiinflammatory activity in rat PBMC assessed as inhibition of LPS-induced TNFalpha production after 20 hrs by ELISA
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type PBMC
Confidence 1 — Organism
Curated By Autocuration

Target

PBMC (CHEMBL613107)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists.
Beattie D, Brearley A, Brown Z, Charlton SJ, Cox B, Fairhurst RA, Fozard JR, Gedeck P, Kirkham P, Meja K, Nanson L, Neef J, Oakman H, Spooner G, Taylor RJ, Turner RJ, West R, Woodward H.
Bioorg Med Chem Lett (2010) 20 : 1219 -1224
PubMed 20031406 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.79 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL186113 GW-328267 1.0 1 8.54
CHEMBL331372 CGS-21680 1 7.08
CHEMBL464859 NECA 1 6.73
CHEMBL592541 1 6.59
CHEMBL592540 1 6.34
CHEMBL604591 1 5.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL186113 GW-328267 IC50 = 2.9 nM 8.54
CHEMBL331372 CGS-21680 IC50 = 83.0 nM 7.08
CHEMBL464859 NECA IC50 = 187.0 nM 6.73
CHEMBL592541 IC50 = 255.0 nM 6.59
CHEMBL592540 IC50 = 458.0 nM 6.34
CHEMBL604591 IC50 = 3591.0 nM 5.45