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Assay Detail

CHEMBL2014359

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

Binding
Displacement of [3H]R-PIA from human recombinant adenosine receptor-1 expressed in CHO cell membrane after 60 mins by liquid scintillation counting
19
Total Activities
19
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 A1 (CHEMBL226)
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 19 6.59 7.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2012686 1 7.32
CHEMBL2012674 1 7.29
CHEMBL2012684 1 7.17
CHEMBL2012682 1 7.14
CHEMBL2012681 1 7.14
CHEMBL2012683 1 7.10
CHEMBL2012678 1 7.08
CHEMBL2012685 1 7.06
CHEMBL2012675 1 6.85
CHEMBL2012679 1 6.70
CHEMBL2012673 1 6.68
CHEMBL2012676 1 6.64
CHEMBL2012672 1 6.46
CHEMBL2012677 1 6.12
CHEMBL2012680 1 6.03
CHEMBL2012691 1 5.90
CHEMBL2012693 1 5.72
CHEMBL2012690 1 5.45
CHEMBL2012687 1 5.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2012686 Ki = 47.9 nM 7.32
CHEMBL2012674 Ki = 51.6 nM 7.29
CHEMBL2012684 Ki = 68.4 nM 7.17
CHEMBL2012682 Ki = 72.2 nM 7.14
CHEMBL2012681 Ki = 72.7 nM 7.14
CHEMBL2012683 Ki = 78.8 nM 7.10
CHEMBL2012678 Ki = 82.6 nM 7.08
CHEMBL2012685 Ki = 86.8 nM 7.06
CHEMBL2012675 Ki = 140.0 nM 6.85
CHEMBL2012679 Ki = 200.0 nM 6.70
CHEMBL2012673 Ki = 210.0 nM 6.68
CHEMBL2012676 Ki = 230.0 nM 6.64
CHEMBL2012672 Ki = 350.0 nM 6.46
CHEMBL2012677 Ki = 760.0 nM 6.12
CHEMBL2012680 Ki = 930.0 nM 6.03
CHEMBL2012691 Ki = 1260.0 nM 5.90
CHEMBL2012693 Ki = 1910.0 nM 5.72
CHEMBL2012690 Ki = 3580.0 nM 5.45
CHEMBL2012687 Ki = 4790.0 nM 5.32