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Assay Detail

CHEMBL645452

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

Binding
Binding affinity for adenosine A2 receptor using [3H]NECA in rat striatal membrane
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Striatum
Subcellular Membrane
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Adenosine A2 receptor (CHEMBL2094117)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists.
van Galen PJ, Nissen P, van Wijngaarden I, IJzerman AP, Soudijn W.
J Med Chem (1991) 34 : 1202 -1206
PubMed 2002461 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.02 6.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19305 1 6.54
CHEMBL276138 1 6.54
CHEMBL19095 1 6.35
CHEMBL19768 1 6.35
CHEMBL19970 1 6.13
CHEMBL1907708 1 6.09
CHEMBL62350 8-PHENYL THEOPHYLLINE 1 6.07
CHEMBL1907924 1 5.55
CHEMBL1355736 THEOPHYLLINE 4.0 1 4.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19305 Ki = 290.0 nM 6.54
CHEMBL276138 Ki = 290.0 nM 6.54
CHEMBL19095 Ki = 450.0 nM 6.35
CHEMBL19768 Ki = 450.0 nM 6.35
CHEMBL19970 Ki = 740.0 nM 6.13
CHEMBL1907708 Ki = 810.0 nM 6.09
CHEMBL62350 8-PHENYL THEOPHYLLINE Ki = 850.0 nM 6.07
CHEMBL1907924 Ki = 2800.0 nM 5.55
CHEMBL1355736 THEOPHYLLINE Ki = 25000.0 nM 4.60