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Assay Detail

CHEMBL923557

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

Binding
Displacement of radioligand from human adenosine A3 receptor expressed in CHO cells
23
Total Activities
23
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 of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.
Melman A, Gao ZG, Kumar D, Wan TC, Gizewski E, Auchampach JA, Jacobson KA.
Bioorg Med Chem Lett (2008) 18 : 2813 -2819
PubMed 18424135 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 8.72 9.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175543 1 9.54
CHEMBL2368455 1 9.42
CHEMBL2368366 1 9.16
CHEMBL2112163 1 9.11
CHEMBL258421 1 9.09
CHEMBL257405 1 9.01
CHEMBL436649 1 8.93
CHEMBL255907 1 8.89
CHEMBL402574 1 8.89
CHEMBL431733 NAMODENOSON 3.0 1 8.85
CHEMBL2112157 1 8.85
CHEMBL27376 1 8.82
CHEMBL2112161 1 8.82
CHEMBL119709 IB-MECA 1 8.76
CHEMBL283057 1 8.66
CHEMBL257785 1 8.66
CHEMBL257833 1 8.62
CHEMBL257573 1 8.54
CHEMBL2112162 1 8.54
CHEMBL2368367 1 8.44
CHEMBL256312 1 8.28
CHEMBL256520 1 7.77
CHEMBL402607 1 6.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175543 Ki = 0.29 nM 9.54
CHEMBL2368455 Ki = 0.38 nM 9.42
CHEMBL2368366 Ki = 0.69 nM 9.16
CHEMBL2112163 Ki = 0.78 nM 9.11
CHEMBL258421 Ki = 0.82 nM 9.09
CHEMBL257405 Ki = 0.98 nM 9.01
CHEMBL436649 Ki = 1.17 nM 8.93
CHEMBL255907 Ki = 1.3 nM 8.89
CHEMBL402574 Ki = 1.3 nM 8.89
CHEMBL431733 NAMODENOSON Ki = 1.4 nM 8.85
CHEMBL2112157 Ki = 1.4 nM 8.85
CHEMBL27376 Ki = 1.5 nM 8.82
CHEMBL2112161 Ki = 1.5 nM 8.82
CHEMBL119709 IB-MECA Ki = 1.74 nM 8.76
CHEMBL283057 Ki = 2.2 nM 8.66
CHEMBL257785 Ki = 2.17 nM 8.66
CHEMBL257833 Ki = 2.38 nM 8.62
CHEMBL257573 Ki = 2.88 nM 8.54
CHEMBL2112162 Ki = 2.9 nM 8.54
CHEMBL2368367 Ki = 3.6 nM 8.44
CHEMBL256312 Ki = 5.21 nM 8.28
CHEMBL256520 Ki = 17.1 nM 7.77
CHEMBL402607 Ki = 149.0 nM 6.83