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

CHEMBL640322

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

Binding
Inhibition of Adenylate cyclase activity in rat fat cell membrane at adenosine A1 receptor
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A1 (CHEMBL318)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives.
Cristalli G, Franchetti P, Grifantini M, Vittori S, Klotz KN, Lohse MJ.
J Med Chem (1988) 31 : 1179 -1183
PubMed 3373486 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.22 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL139000 (R)-PIA 1 7.40
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 7.24
CHEMBL464859 NECA 1 6.70
CHEMBL2113390 1 6.44
CHEMBL606016 1 6.20
CHEMBL605008 1 6.02
CHEMBL2113389 1 6.01
CHEMBL2113396 1 5.82
CHEMBL2113387 1 5.80
CHEMBL2113391 1 5.62
CHEMBL115824 1 5.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL139000 (R)-PIA IC50 = 40.0 nM 7.40
CHEMBL68738 N6-CYCLOPENTYLADENOSINE IC50 = 58.0 nM 7.24
CHEMBL464859 NECA IC50 = 200.0 nM 6.70
CHEMBL2113390 IC50 = 360.0 nM 6.44
CHEMBL606016 IC50 = 630.0 nM 6.20
CHEMBL605008 IC50 = 960.0 nM 6.02
CHEMBL2113389 IC50 = 970.0 nM 6.01
CHEMBL2113396 IC50 = 1500.0 nM 5.82
CHEMBL2113387 IC50 = 1600.0 nM 5.80
CHEMBL2113391 IC50 = 2400.0 nM 5.62
CHEMBL115824 IC50 = 6700.0 nM 5.17