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Assay Detail

CHEMBL649877

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

Binding
Binding affinity against Adenosine A2 receptor in rat striatum by displacement of [3H]N-ethyladenosine-5''-uronamide(NECA)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

1,3,8-trisubstituted xanthines. Effects of substitution pattern upon adenosine receptor A1/A2 affinity.
Erickson RH, Hiner RN, Feeney SW, Blake PR, Rzeszotarski WJ, Hicks RP, Costello DG, Abreu ME.
J Med Chem (1991) 34 : 1431 -1435
PubMed 2016719 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.35 7.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL286347 1 7.15
CHEMBL33722 1 6.76
CHEMBL33169 1 6.50
CHEMBL287010 1 6.46
CHEMBL33893 1 6.14
CHEMBL284598 1 5.92
CHEMBL285212 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL286347 Ki = 70.3 nM 7.15
CHEMBL33722 Ki = 173.0 nM 6.76
CHEMBL33169 Ki = 315.0 nM 6.50
CHEMBL287010 Ki = 347.0 nM 6.46
CHEMBL33893 Ki = 719.0 nM 6.14
CHEMBL284598 Ki = 1200.0 nM 5.92
CHEMBL285212 Ki = 3100.0 nM 5.51