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Assay Detail

CHEMBL910041

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

Binding
Displacement of [125I]ABA from human adenosine A1 receptor
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A1 (CHEMBL226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tricyclic imidazoline derivatives as potent and selective adenosine A1 receptor antagonists.
Vu CB, Kiesman WF, Conlon PR, Lin KC, Tam M, Petter RC, Smits G, Lutterodt F, Jin X, Chen L, Zhang J.
J Med Chem (2006) 49 : 7132 -7139
PubMed 17125265 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.71 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL218458 1 8.70
CHEMBL414157 TONAPOFYLLINE 3.0 1 8.15
CHEMBL450341 1 7.66
CHEMBL217268 1 7.46
CHEMBL216269 1 7.46
CHEMBL216200 1 7.35
CHEMBL384279 1 7.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL218458 Ki = 2.0 nM 8.70
CHEMBL414157 TONAPOFYLLINE Ki = 7.0 nM 8.15
CHEMBL450341 Ki = 22.0 nM 7.66
CHEMBL217268 Ki = 35.0 nM 7.46
CHEMBL216269 Ki = 35.0 nM 7.46
CHEMBL216200 Ki = 45.0 nM 7.35
CHEMBL384279 Ki = 60.0 nM 7.22