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Assay Detail

CHEMBL2014402

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

Binding
Displacement of [125I]AB-MECA from human recombinant adenosine receptor-3 expressed in CHO cell membrane after 60 mins by gamma-counting
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Truncated (N)-Methanocarba Nucleosides as A(1) Adenosine Receptor Agonists and Partial Agonists: Overcoming Lack of a Recognition Element.
Tosh DK, Phan K, Deflorian F, Wei Q, Gao ZG, Jacobson KA.
ACS Med Chem Lett (2011) 2 : 626 -631
PubMed 21858244 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 7.23 8.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2012674 1 8.23
CHEMBL2012680 1 8.18
CHEMBL2012684 1 8.05
CHEMBL2012688 1 7.99
CHEMBL2012673 1 7.92
CHEMBL2012682 1 7.92
CHEMBL2012689 1 7.82
CHEMBL2012691 1 7.78
CHEMBL2012681 1 7.49
CHEMBL2012693 1 7.39
CHEMBL2012687 1 7.38
CHEMBL2012683 1 7.28
CHEMBL2012692 1 7.08
CHEMBL2012685 1 6.96
CHEMBL2012690 1 6.94
CHEMBL2012672 1 6.80
CHEMBL2012679 1 6.63
CHEMBL2012678 1 6.50
CHEMBL2012686 1 6.33
CHEMBL2012675 1 6.30
CHEMBL2012676 1 6.25
CHEMBL2012677 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2012674 Ki = 5.9 nM 8.23
CHEMBL2012680 Ki = 6.6 nM 8.18
CHEMBL2012684 Ki = 8.9 nM 8.05
CHEMBL2012688 Ki = 10.3 nM 7.99
CHEMBL2012673 Ki = 12.1 nM 7.92
CHEMBL2012682 Ki = 12.0 nM 7.92
CHEMBL2012689 Ki = 15.2 nM 7.82
CHEMBL2012691 Ki = 16.5 nM 7.78
CHEMBL2012681 Ki = 32.4 nM 7.49
CHEMBL2012693 Ki = 40.4 nM 7.39
CHEMBL2012687 Ki = 41.5 nM 7.38
CHEMBL2012683 Ki = 52.0 nM 7.28
CHEMBL2012692 Ki = 83.2 nM 7.08
CHEMBL2012685 Ki = 110.0 nM 6.96
CHEMBL2012690 Ki = 114.0 nM 6.94
CHEMBL2012672 Ki = 160.0 nM 6.80
CHEMBL2012679 Ki = 236.0 nM 6.63
CHEMBL2012678 Ki = 315.0 nM 6.50
CHEMBL2012686 Ki = 470.0 nM 6.33
CHEMBL2012675 Ki = 500.0 nM 6.30
CHEMBL2012676 Ki = 560.0 nM 6.25
CHEMBL2012677 Ki = 1530.0 nM 5.82