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Assay Detail

CHEMBL841776

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

Binding
Displacement of [3H]DPCPX binding to human adenosine A1 receptor expressed in CHO cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A1 (CHEMBL226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor.
Chang LC, von Frijtag Drabbe Künzel JK, Mulder-Krieger T, Spanjersberg RF, Roerink SF, van den Hout G, Beukers MW, Brussee J, Ijzerman AP.
J Med Chem (2005) 48 : 2045 -2053
PubMed 15771447 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.43 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL176254 1 8.37
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 8.21
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 8.00
CHEMBL176295 1 7.96
CHEMBL175787 1 7.92
CHEMBL359833 1 7.85
CHEMBL361531 1 7.82
CHEMBL175788 1 7.64
CHEMBL179358 1 7.52
CHEMBL179299 1 7.47
CHEMBL179198 1 7.40
CHEMBL368237 1 7.40
CHEMBL176060 1 7.39
CHEMBL447487 1 7.31
CHEMBL178932 1 7.09
CHEMBL179300 1 7.09
CHEMBL177571 1 6.82
CHEMBL179684 1 6.81
CHEMBL175990 1 6.61
CHEMBL48278 1 5.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL176254 Ki = 4.3 nM 8.37
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 6.1 nM 8.21
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 10.0 nM 8.00
CHEMBL176295 Ki = 11.0 nM 7.96
CHEMBL175787 Ki = 12.0 nM 7.92
CHEMBL359833 Ki = 14.0 nM 7.85
CHEMBL361531 Ki = 15.0 nM 7.82
CHEMBL175788 Ki = 23.0 nM 7.64
CHEMBL179358 Ki = 30.0 nM 7.52
CHEMBL179299 Ki = 34.0 nM 7.47
CHEMBL179198 Ki = 40.0 nM 7.40
CHEMBL368237 Ki = 40.0 nM 7.40
CHEMBL176060 Ki = 41.0 nM 7.39
CHEMBL447487 Ki = 49.0 nM 7.31
CHEMBL178932 Ki = 81.0 nM 7.09
CHEMBL179300 Ki = 81.0 nM 7.09
CHEMBL177571 Ki = 150.0 nM 6.82
CHEMBL179684 Ki = 156.0 nM 6.81
CHEMBL175990 Ki = 245.0 nM 6.61
CHEMBL48278 Ki = 1081.0 nM 5.97