Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL642308

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

Binding
Binding affinity towards adenosine A1 receptor in rat cerebral cortical membranes by [3H]cyclohexyladenosine displacement.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Functionalized congeners of 1,3-dialkylxanthines: preparation of analogues with high affinity for adenosine receptors.
Jacobson KA, Kirk KL, Padgett WL, Daly JW.
J Med Chem (1985) 28 : 1334 -1340
PubMed 2993622 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.69 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL273094 XANTHINE AMINE CONGENER 1 8.92
CHEMBL286728 1 8.66
CHEMBL27155 1 8.54
CHEMBL444281 1 8.39
CHEMBL422937 1 8.30
CHEMBL27081 1 8.05
CHEMBL265739 1 7.62
CHEMBL441598 1 7.58
CHEMBL27028 1 7.50
CHEMBL432664 1 7.44
CHEMBL27762 1 7.38
CHEMBL27047 1 7.30
CHEMBL283628 1 7.27
CHEMBL27041 1 7.24
CHEMBL286063 1 7.23
CHEMBL286493 1 7.02
CHEMBL285103 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL273094 XANTHINE AMINE CONGENER Ki = 1.2 nM 8.92
CHEMBL286728 Ki = 2.2 nM 8.66
CHEMBL27155 Ki = 2.9 nM 8.54
CHEMBL444281 Ki = 4.1 nM 8.39
CHEMBL422937 Ki = 5.0 nM 8.30
CHEMBL27081 Ki = 9.0 nM 8.05
CHEMBL265739 Ki = 24.0 nM 7.62
CHEMBL441598 Ki = 26.0 nM 7.58
CHEMBL27028 Ki = 32.0 nM 7.50
CHEMBL432664 Ki = 36.0 nM 7.44
CHEMBL27762 Ki = 42.0 nM 7.38
CHEMBL27047 Ki = 50.0 nM 7.30
CHEMBL283628 Ki = 54.0 nM 7.27
CHEMBL27041 Ki = 58.0 nM 7.24
CHEMBL286063 Ki = 59.0 nM 7.23
CHEMBL286493 Ki = 96.0 nM 7.02
CHEMBL285103 Ki = 500.0 nM 6.30