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Assay Detail

CHEMBL641719

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

Binding
Binding affinity at Adenosine A1 receptor in rat brain membranes by [3H](R)-PIA displacement.
17
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Brain membranes
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

New base-altered adenosine analogues: Synthesis and affinity at adenosine A1 and A2A receptors
Ha SB, Melman N, Jacobson KA, Nair V
Bioorg Med Chem Lett (1997) 7 : 3085 -3090
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.31 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL88439 1 9.05
CHEMBL610971 1 8.62
CHEMBL321536 1 8.57
CHEMBL423315 1 8.45
CHEMBL313306 1 8.31
CHEMBL313806 1 8.14
CHEMBL104580 2 8.10
CHEMBL611882 1 7.64
CHEMBL610970 1 7.15
CHEMBL607753 1 6.95
CHEMBL607752 1 6.86
CHEMBL608330 1 6.65
CHEMBL612197 1 6.34
CHEMBL610401 1 6.00
CHEMBL610681 1 4.81
CHEMBL236757 1 4.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL88439 Ki = 0.9 nM 9.05
CHEMBL610971 Ki = 2.41 nM 8.62
CHEMBL321536 Ki = 2.7 nM 8.57
CHEMBL423315 Ki = 3.55 nM 8.45
CHEMBL313306 Ki = 4.89 nM 8.31
CHEMBL313806 Ki = 7.3 nM 8.14
CHEMBL104580 Ki = 8.0 nM 8.10
CHEMBL104580 Ki = 8.0 nM 8.10
CHEMBL611882 Ki = 23.0 nM 7.64
CHEMBL610970 Ki = 71.0 nM 7.15
CHEMBL607753 Ki = 113.0 nM 6.95
CHEMBL607752 Ki = 139.0 nM 6.86
CHEMBL608330 Ki = 224.0 nM 6.65
CHEMBL612197 Ki = 452.0 nM 6.34
CHEMBL610401 Ki = 989.0 nM 6.00
CHEMBL610681 Ki = 15500.0 nM 4.81
CHEMBL236757 Ki = 29700.0 nM 4.53