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Assay Detail

CHEMBL641336

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Binding
Inhibition of [125I]I-AB-MECA binding to human Adenosine A3 receptor
10
Total Activities
10
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 A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.
Kim SA, Marshall MA, Melman N, Kim HS, Müller CE, Linden J, Jacobson KA.
J Med Chem (2002) 45 : 2131 -2138
PubMed 12014951 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 5.61 8.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68278 1 8.34
CHEMBL302344 1 6.19
CHEMBL39986 1 5.62
CHEMBL67415 1 5.51
CHEMBL63944 1 5.35
CHEMBL67228 1 5.16
CHEMBL67949 1 5.12
CHEMBL67313 1 5.06
CHEMBL304455 1 4.96
CHEMBL66899 1 4.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68278 Ki = 4.61 nM 8.34
CHEMBL302344 Ki = 639.0 nM 6.19
CHEMBL39986 Ki = 2370.0 nM 5.62
CHEMBL67415 Ki = 3080.0 nM 5.51
CHEMBL63944 Ki = 4440.0 nM 5.35
CHEMBL67228 Ki = 6880.0 nM 5.16
CHEMBL67949 Ki = 7510.0 nM 5.12
CHEMBL67313 Ki = 8650.0 nM 5.06
CHEMBL304455 Ki = 10900.0 nM 4.96
CHEMBL66899 Ki = 16100.0 nM 4.79