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Assay Detail

CHEMBL644771

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

Binding
Binding affinity to A2 adenosine receptor in rat striatal membranes by [3H]NECA (1-(6-amino-9H-purin-9-yl)-1-deoxy-N-ethyl-beta-D-ribofuranuronamide) displacement.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

N6-(2,2-diphenylethyl)adenosine, a novel adenosine receptor agonist with antipsychotic-like activity.
Bridges AJ, Moos WH, Szotek DL, Trivedi BK, Bristol JA, Heffner TG, Bruns RF, Downs DA.
J Med Chem (1987) 30 : 1709 -1711
PubMed 2888894 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.29 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL193692 1 7.60
CHEMBL606505 1 7.52
CHEMBL2094078 1 7.01
CHEMBL139000 (R)-PIA 1 6.91
CHEMBL1257013 1 6.79
CHEMBL388757 N6-BENZYLADENOSINE 1 6.55
CHEMBL606073 1 6.54
CHEMBL604410 1 6.50
CHEMBL2113484 1 6.38
CHEMBL262083 N6-PHENYLADENOSINE 1 6.18
CHEMBL2113406 1 5.91
CHEMBL420705 (S)-PIA 1 5.76
CHEMBL603570 1 5.66
CHEMBL606064 1 5.42
CHEMBL610070 1 5.33
CHEMBL605457 1 4.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL193692 Ki = 25.0 nM 7.60
CHEMBL606505 Ki = 30.0 nM 7.52
CHEMBL2094078 Ki = 98.0 nM 7.01
CHEMBL139000 (R)-PIA Ki = 124.0 nM 6.91
CHEMBL1257013 Ki = 161.0 nM 6.79
CHEMBL388757 N6-BENZYLADENOSINE Ki = 280.0 nM 6.55
CHEMBL606073 Ki = 290.0 nM 6.54
CHEMBL604410 Ki = 320.0 nM 6.50
CHEMBL2113484 Ki = 420.0 nM 6.38
CHEMBL262083 N6-PHENYLADENOSINE Ki = 660.0 nM 6.18
CHEMBL2113406 Ki = 1230.0 nM 5.91
CHEMBL420705 (S)-PIA Ki = 1720.0 nM 5.76
CHEMBL603570 Ki = 2200.0 nM 5.66
CHEMBL606064 Ki = 3800.0 nM 5.42
CHEMBL610070 Ki = 4700.0 nM 5.33
CHEMBL605457 Ki = 26000.0 nM 4.58