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Assay Detail

CHEMBL640363

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

Binding
Displacement of [3H]DPCPX from adenosine A1 receptor of rat brain cortical membrane
8
Total Activities
8
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

Isoquinoline and quinazoline urea analogues as antagonists for the human adenosine A(3) receptor.
van Muijlwijk-Koezen JE, Timmerman H, van der Goot H, Menge WM, Frijtag Von Drabbe Künzel J, de Groote M, IJzerman AP.
J Med Chem (2000) 43 : 2227 -2238
PubMed 10841801 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.10 6.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL72287 1 6.62
CHEMBL71053 1 5.50
CHEMBL305516 1 4.19
CHEMBL305975 1 4.07
CHEMBL305512 1 -
CHEMBL308087 1 -
CHEMBL72183 1 -
CHEMBL72172 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL72287 Ki = 240.0 nM 6.62
CHEMBL71053 Ki = 3200.0 nM 5.50
CHEMBL305516 Ki = 64800.0 nM 4.19
CHEMBL305975 Ki = 84500.0 nM 4.07
CHEMBL305512 Ki = 170000.0 nM -
CHEMBL308087 Ki = 3870000.0 nM -
CHEMBL72183 Ki = 166000.0 nM -
CHEMBL72172 Ki = 295000.0 nM -