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Assay Detail

CHEMBL641069

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

Binding
Displacement of [3H]-CCPA from adenosine A1 receptor of rat brain cortical membrane preparations
13
Total Activities
13
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

Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability.
Yan L, Müller CE.
J Med Chem (2004) 47 : 1031 -1043
PubMed 14761205 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.83 8.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL412854 1 8.59
CHEMBL8865 1 8.57
CHEMBL8732 1 8.44
CHEMBL266099 1 8.36
CHEMBL8810 1 8.24
CHEMBL417601 1 8.20
CHEMBL8495 1 8.19
CHEMBL9030 1 8.11
CHEMBL267474 1 7.75
CHEMBL9034 1 7.68
CHEMBL8789 1 7.40
CHEMBL268617 1 6.32
CHEMBL8565 1 5.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL412854 Ki = 2.6 nM 8.59
CHEMBL8865 Ki = 2.7 nM 8.57
CHEMBL8732 Ki = 3.6 nM 8.44
CHEMBL266099 Ki = 4.4 nM 8.36
CHEMBL8810 Ki = 5.7 nM 8.24
CHEMBL417601 Ki = 6.3 nM 8.20
CHEMBL8495 Ki = 6.5 nM 8.19
CHEMBL9030 Ki = 7.7 nM 8.11
CHEMBL267474 Ki = 18.0 nM 7.75
CHEMBL9034 Ki = 21.0 nM 7.68
CHEMBL8789 Ki = 40.0 nM 7.40
CHEMBL268617 Ki = 475.0 nM 6.32
CHEMBL8565 Ki = 1238.0 nM 5.91