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Assay Detail

CHEMBL908370

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Functional
Intrinsic activity at adenosine A1 receptor assessed as blockade of CPA in isolated spontaneously beating rat atria
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

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
Kd 3 9.53 9.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL216269 1 9.90
CHEMBL414157 TONAPOFYLLINE 3.0 1 9.80
CHEMBL450341 1 8.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL216269 Kd = 0.1259 nM 9.90
CHEMBL414157 TONAPOFYLLINE Kd = 0.1585 nM 9.80
CHEMBL450341 Kd = 1.318 nM 8.88