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Assay Detail

CHEMBL1070691

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

Binding
Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in CHO cells
10
Total Activities
10
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 A2a (CHEMBL251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of N(6)-substituted-4'-thioadenosine-5'-uronamides as potent and selective human A(3) adenosine receptor agonists.
Choi WJ, Lee HW, Kim HO, Chinn M, Gao ZG, Patel A, Jacobson KA, Moon HR, Jung YH, Jeong LS.
Bioorg Med Chem (2009) 17 : 8003 -8011
PubMed 19879151 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 6.53 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL596014 1 7.82
CHEMBL596042 1 7.24
CHEMBL606630 1 6.97
CHEMBL594625 1 6.91
CHEMBL596460 1 6.79
CHEMBL200732 1 6.65
CHEMBL522152 1 6.32
CHEMBL603424 1 5.80
CHEMBL119709 IB-MECA 1 5.54
CHEMBL431733 NAMODENOSON 3.0 1 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL596014 Ki = 15.2 nM 7.82
CHEMBL596042 Ki = 57.6 nM 7.24
CHEMBL606630 Ki = 108.0 nM 6.97
CHEMBL594625 Ki = 122.0 nM 6.91
CHEMBL596460 Ki = 161.0 nM 6.79
CHEMBL200732 Ki = 223.0 nM 6.65
CHEMBL522152 Ki = 475.0 nM 6.32
CHEMBL603424 Ki = 1600.0 nM 5.80
CHEMBL119709 IB-MECA Ki = 2900.0 nM 5.54
CHEMBL431733 NAMODENOSON Ki = 5360.0 nM 5.27