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Assay Detail

CHEMBL641718

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

Binding
Displacement of [3H]DPCPX from rat cortical membranes Adenosine A1 receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

N6,5'-Disubstituted adenosine derivatives as partial agonists for the human adenosine A3 receptor.
van Tilburg EW, von Frijtag Drabbe Künzel J, de Groote M, Vollinga RC, Lorenzen A, IJzerman AP.
J Med Chem (1999) 42 : 1393 -1400
PubMed 10212125 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.83 8.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 8.23
CHEMBL477444 1 8.02
CHEMBL2113425 1 7.39
CHEMBL263643 1 7.35
CHEMBL2113468 1 7.23
CHEMBL2113467 1 7.12
CHEMBL66393 1 7.10
CHEMBL2113422 1 6.57
CHEMBL2113427 1 6.21
CHEMBL2113428 1 6.14
CHEMBL388757 N6-BENZYLADENOSINE 1 5.35
CHEMBL2113429 1 5.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 5.9 nM 8.23
CHEMBL477444 Ki = 9.5 nM 8.02
CHEMBL2113425 Ki = 41.0 nM 7.39
CHEMBL263643 Ki = 45.0 nM 7.35
CHEMBL2113468 Ki = 59.0 nM 7.23
CHEMBL2113467 Ki = 76.0 nM 7.12
CHEMBL66393 Ki = 78.8 nM 7.10
CHEMBL2113422 Ki = 270.0 nM 6.57
CHEMBL2113427 Ki = 610.0 nM 6.21
CHEMBL2113428 Ki = 720.0 nM 6.14
CHEMBL388757 N6-BENZYLADENOSINE Ki = 4450.0 nM 5.35
CHEMBL2113429 Ki = 5875.0 nM 5.23