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Assay Detail

CHEMBL640268

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

Binding
Displacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A2b (CHEMBL255)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists.
Jacobson KA, Ji X, Li AH, Melman N, Siddiqui MA, Shin KJ, Marquez VE, Ravi RG.
J Med Chem (2000) 43 : 2196 -2203
PubMed 10841798 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 4.82 5.45

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL66393 1 5.45
CHEMBL307199 1 5.30
CHEMBL417292 1 4.92
CHEMBL284969 1 4.69
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 4.67
CHEMBL27809 1 4.39
CHEMBL49935 ARISTEROMYCIN 1 4.33
CHEMBL27952 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL66393 Ki = 3570.0 nM 5.45
CHEMBL307199 Ki = 5010.0 nM 5.30
CHEMBL417292 Ki = 12100.0 nM 4.92
CHEMBL284969 Ki = 20400.0 nM 4.69
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 21200.0 nM 4.67
CHEMBL27809 Ki = 41000.0 nM 4.39
CHEMBL49935 ARISTEROMYCIN Ki = 47300.0 nM 4.33
CHEMBL27952 Ki = 139000.0 nM -