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Assay Detail

CHEMBL1070693

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

Binding
Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells
27
Total Activities
27
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

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 27 8.12 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL522152 1 9.60
CHEMBL201706 1 9.55
CHEMBL200732 1 9.42
CHEMBL596042 1 9.38
CHEMBL595569 1 9.01
CHEMBL611359 1 9.01
CHEMBL119709 IB-MECA 1 9.00
CHEMBL606630 1 8.98
CHEMBL594625 1 8.93
CHEMBL608680 1 8.92
CHEMBL594619 1 8.87
CHEMBL431733 NAMODENOSON 3.0 1 8.85
CHEMBL596460 1 8.67
CHEMBL603424 1 8.67
CHEMBL596014 1 8.52
CHEMBL603643 1 7.81
CHEMBL604790 1 7.51
CHEMBL595117 1 7.45
CHEMBL593958 1 7.21
CHEMBL596027 1 7.02
CHEMBL596269 1 7.01
CHEMBL594577 1 6.95
CHEMBL593445 1 6.94
CHEMBL593468 1 6.87
CHEMBL593724 1 6.84
CHEMBL595987 1 6.36
CHEMBL594620 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL522152 Ki = 0.25 nM 9.60
CHEMBL201706 Ki = 0.28 nM 9.55
CHEMBL200732 Ki = 0.38 nM 9.42
CHEMBL596042 Ki = 0.42 nM 9.38
CHEMBL595569 Ki = 0.97 nM 9.01
CHEMBL611359 Ki = 0.97 nM 9.01
CHEMBL119709 IB-MECA Ki = 1.0 nM 9.00
CHEMBL606630 Ki = 1.04 nM 8.98
CHEMBL594625 Ki = 1.17 nM 8.93
CHEMBL608680 Ki = 1.19 nM 8.92
CHEMBL594619 Ki = 1.35 nM 8.87
CHEMBL431733 NAMODENOSON Ki = 1.4 nM 8.85
CHEMBL596460 Ki = 2.16 nM 8.67
CHEMBL603424 Ki = 2.16 nM 8.67
CHEMBL596014 Ki = 3.03 nM 8.52
CHEMBL603643 Ki = 15.6 nM 7.81
CHEMBL604790 Ki = 31.0 nM 7.51
CHEMBL595117 Ki = 35.4 nM 7.45
CHEMBL593958 Ki = 61.1 nM 7.21
CHEMBL596027 Ki = 94.9 nM 7.02
CHEMBL596269 Ki = 97.0 nM 7.01
CHEMBL594577 Ki = 113.0 nM 6.95
CHEMBL593445 Ki = 116.0 nM 6.94
CHEMBL593468 Ki = 135.0 nM 6.87
CHEMBL593724 Ki = 144.0 nM 6.84
CHEMBL595987 Ki = 433.0 nM 6.36
CHEMBL594620 Ki = 1200.0 nM 5.92