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Assay Detail

CHEMBL641960

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

Binding
Displacement of [3H]AB-MECA from human Adenosine A3 receptor expressed in HEK cells
14
Total Activities
14
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 A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective A(3) adenosine receptor antagonists: water-soluble 3, 5-diacyl-1,2,4-trialkylpyridinium salts and their oxidative generation from dihydropyridine precursors.
Xie R, Li AH, Ji XD, Melman N, Olah ME, Stiles GL, Jacobson KA.
J Med Chem (1999) 42 : 4232 -4238
PubMed 10514293 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.21 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL436180 1 6.66
CHEMBL135569 1 6.46
CHEMBL277079 1 6.44
CHEMBL135361 1 6.42
CHEMBL337088 1 6.36
CHEMBL424079 1 6.33
CHEMBL135356 1 6.32
CHEMBL274501 1 6.27
CHEMBL135323 1 6.24
CHEMBL335740 1 6.16
CHEMBL337503 1 5.90
CHEMBL336629 1 5.87
CHEMBL340552 1 5.85
CHEMBL440720 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL436180 Ki = 219.0 nM 6.66
CHEMBL135569 Ki = 348.0 nM 6.46
CHEMBL277079 Ki = 364.0 nM 6.44
CHEMBL135361 Ki = 379.0 nM 6.42
CHEMBL337088 Ki = 436.0 nM 6.36
CHEMBL424079 Ki = 465.0 nM 6.33
CHEMBL135356 Ki = 483.0 nM 6.32
CHEMBL274501 Ki = 538.0 nM 6.27
CHEMBL135323 Ki = 577.0 nM 6.24
CHEMBL335740 Ki = 695.0 nM 6.16
CHEMBL337503 Ki = 1250.0 nM 5.90
CHEMBL336629 Ki = 1350.0 nM 5.87
CHEMBL340552 Ki = 1410.0 nM 5.85
CHEMBL440720 Ki = 2020.0 nM 5.70