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Assay Detail

CHEMBL642476

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Binding
Evaluated for binding affinity against Adenosine A1 receptor
19
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

A steric and electrostatic comparison of three models for the agonist/antagonist binding site on the adenosine A1 receptor.
van der Wenden EM, Ijzerman AP, Soudijn W.
J Med Chem (1992) 35 : 629 -635
PubMed 1542091 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 8.19 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 9.49
CHEMBL45891 1 9.07
CHEMBL607777 1 9.00
CHEMBL611903 2 8.92
CHEMBL610427 1 8.70
CHEMBL2113423 1 8.68
CHEMBL612218 1 8.66
CHEMBL262083 N6-PHENYLADENOSINE 1 8.48
CHEMBL608952 1 8.40
CHEMBL1093910 2 8.34
CHEMBL605042 1 8.31
CHEMBL607776 1 8.05
CHEMBL612221 1 7.57
CHEMBL604407 1 7.40
CHEMBL608355 1 7.33
CHEMBL604860 1 7.07
CHEMBL388757 N6-BENZYLADENOSINE 1 6.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE IC50 = 0.3236 nM 9.49
CHEMBL45891 IC50 = 0.8511 nM 9.07
CHEMBL607777 IC50 = 1.0 nM 9.00
CHEMBL611903 IC50 = 1.202 nM 8.92
CHEMBL610427 IC50 = 1.995 nM 8.70
CHEMBL2113423 IC50 = 2.089 nM 8.68
CHEMBL612218 IC50 = 2.188 nM 8.66
CHEMBL262083 N6-PHENYLADENOSINE IC50 = 3.311 nM 8.48
CHEMBL608952 IC50 = 3.981 nM 8.40
CHEMBL1093910 IC50 = 4.571 nM 8.34
CHEMBL605042 IC50 = 4.898 nM 8.31
CHEMBL607776 IC50 = 8.913 nM 8.05
CHEMBL1093910 IC50 = 8.913 nM 8.05
CHEMBL612221 IC50 = 26.92 nM 7.57
CHEMBL604407 IC50 = 39.81 nM 7.40
CHEMBL608355 IC50 = 46.77 nM 7.33
CHEMBL611903 IC50 = 52.48 nM 7.28
CHEMBL604860 IC50 = 85.11 nM 7.07
CHEMBL388757 N6-BENZYLADENOSINE IC50 = 125.89 nM 6.90