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Assay Detail

CHEMBL640359

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Binding
Binding affinity for adenosine A1 receptor in rat brain membranes using [3H]CHA as radioligand
18
Total Activities
18
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

Ribose-modified adenosine analogues as adenosine receptor agonists.
Taylor MD, Moos WH, Hamilton HW, Szotek DS, Patt WC, Badger EW, Bristol JA, Bruns RF, Heffner TG, Mertz TE.
J Med Chem (1986) 29 : 346 -353
PubMed 3005574 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.30 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL139000 (R)-PIA 1 8.96
CHEMBL611892 1 8.80
CHEMBL607763 1 7.60
CHEMBL2112569 1 7.54
CHEMBL610691 1 7.54
CHEMBL325664 1 5.92
CHEMBL118802 1 5.82
CHEMBL2112121 1 5.72
CHEMBL332331 1 5.24
CHEMBL118785 1 5.02
CHEMBL331957 1 4.82
CHEMBL2111777 1 4.70
CHEMBL117739 1 4.17
CHEMBL118435 1 -
CHEMBL609528 1 -
CHEMBL325192 1 -
CHEMBL120075 1 -
CHEMBL332668 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL139000 (R)-PIA Ki = 1.1 nM 8.96
CHEMBL611892 Ki = 1.6 nM 8.80
CHEMBL607763 Ki = 25.0 nM 7.60
CHEMBL2112569 Ki = 29.0 nM 7.54
CHEMBL610691 Ki = 29.0 nM 7.54
CHEMBL325664 Ki = 1200.0 nM 5.92
CHEMBL118802 Ki = 1500.0 nM 5.82
CHEMBL2112121 Ki = 1900.0 nM 5.72
CHEMBL332331 Ki = 5700.0 nM 5.24
CHEMBL118785 Ki = 9600.0 nM 5.02
CHEMBL331957 Ki = 15000.0 nM 4.82
CHEMBL2111777 Ki = 20000.0 nM 4.70
CHEMBL117739 Ki = 68000.0 nM 4.17
CHEMBL118435 Ki > 10000.0 nM -
CHEMBL609528 Ki > 10000.0 nM -
CHEMBL325192 Ki > 10000.0 nM -
CHEMBL120075 Ki > 10000.0 nM -
CHEMBL332668 Ki > 2200.0 nM -