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Assay Detail

CHEMBL640343

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

Functional
Inhibition of adenosine induced negative inotropic activity against guinea-pig atria (Adenosine A1 receptor)
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Adenosine receptor A1 (CHEMBL2304404)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Discovery of FK453, a novel non-xanthine adenosine A1 receptor antagonist
Akahane A, Katayama H, Mitsunaga T, Kita Y, Kusunoki T, Terai T, Yoshida K, Shiokawa Y
Bioorg Med Chem Lett (1996) 6 : 2059 -2062
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.02 9.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL61845 1 9.25
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 8.88
CHEMBL440115 FK453 1.0 1 5.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL61845 IC50 = 0.56 nM 9.25
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] IC50 = 1.31 nM 8.88
CHEMBL440115 FK453 IC50 = 1180.0 nM 5.93