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Assay Detail

CHEMBL935757

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

Binding
Displacement of [125I]N6-(-amino-3-iodobenzyl)adenosine-5'-N-methyl-uronamide from mouse recombinant adenosine A3 receptor expressed in HEK293 cells
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A3 (CHEMBL1075269)
Type SINGLE PROTEIN
Organism Mus musculus

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 8.49 10.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL119709 IB-MECA 1 10.06
CHEMBL431733 NAMODENOSON 3.0 1 9.74
CHEMBL27376 1 9.10
CHEMBL402574 1 9.07
CHEMBL2368455 1 9.05
CHEMBL2368367 1 8.93
CHEMBL2112161 1 8.92
CHEMBL175543 1 8.83
CHEMBL255907 1 8.82
CHEMBL2368366 1 8.78
CHEMBL2112157 1 8.76
CHEMBL2112162 1 8.71
CHEMBL2112163 1 8.55
CHEMBL257405 1 8.35
CHEMBL257573 1 8.33
CHEMBL436649 1 8.33
CHEMBL258421 1 8.22
CHEMBL257785 1 8.07
CHEMBL256312 1 7.92
CHEMBL256520 1 7.84
CHEMBL257833 1 7.61
CHEMBL283057 1 7.31
CHEMBL402607 1 6.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL119709 IB-MECA Ki = 0.087 nM 10.06
CHEMBL431733 NAMODENOSON Ki = 0.18 nM 9.74
CHEMBL27376 Ki = 0.8 nM 9.10
CHEMBL402574 Ki = 0.85 nM 9.07
CHEMBL2368455 Ki = 0.9 nM 9.05
CHEMBL2368367 Ki = 1.18 nM 8.93
CHEMBL2112161 Ki = 1.19 nM 8.92
CHEMBL175543 Ki = 1.49 nM 8.83
CHEMBL255907 Ki = 1.51 nM 8.82
CHEMBL2368366 Ki = 1.67 nM 8.78
CHEMBL2112157 Ki = 1.72 nM 8.76
CHEMBL2112162 Ki = 1.94 nM 8.71
CHEMBL2112163 Ki = 2.79 nM 8.55
CHEMBL257405 Ki = 4.46 nM 8.35
CHEMBL257573 Ki = 4.65 nM 8.33
CHEMBL436649 Ki = 4.65 nM 8.33
CHEMBL258421 Ki = 6.06 nM 8.22
CHEMBL257785 Ki = 8.6 nM 8.07
CHEMBL256312 Ki = 11.9 nM 7.92
CHEMBL256520 Ki = 14.4 nM 7.84
CHEMBL257833 Ki = 24.4 nM 7.61
CHEMBL283057 Ki = 49.0 nM 7.31
CHEMBL402607 Ki = 877.0 nM 6.06