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Assay Detail

CHEMBL840054

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

Binding
Displacement of [125I]AB-MECA binding to Adenosine A3 receptor expressed in CHO cells
24
Total Activities
24
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 Expert

Target

Adenosine receptor A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of novel N6-[4-(substituted)sulfonamidophenylcarbamoyl]adenosine-5'-uronamides as A3 adenosine receptor agonists.
Baraldi PG, Fruttarolo F, Tabrizi MA, Romagnoli R, Preti D, Bovero A, Pineda de Las Infantas MJ, Moorman A, Varani K, Borea PA.
J Med Chem (2004) 47 : 5535 -5540
PubMed 15481989 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 7.84 9.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL431733 NAMODENOSON 3.0 1 9.48
CHEMBL119709 IB-MECA 1 8.96
CHEMBL608755 1 8.10
CHEMBL611091 1 8.05
CHEMBL611104 1 8.00
CHEMBL611095 1 8.00
CHEMBL610845 1 7.92
CHEMBL610849 1 7.85
CHEMBL265587 1 7.83
CHEMBL610814 1 7.77
CHEMBL610846 1 7.72
CHEMBL611089 1 7.70
CHEMBL610589 1 7.70
CHEMBL610847 1 7.66
CHEMBL611090 1 7.64
CHEMBL610830 1 7.64
CHEMBL610584 1 7.64
CHEMBL610837 1 7.64
CHEMBL610579 1 7.62
CHEMBL611092 1 7.62
CHEMBL611099 1 7.60
CHEMBL610829 1 7.46
CHEMBL464859 NECA 1 7.46
CHEMBL610580 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL431733 NAMODENOSON Ki = 0.33 nM 9.48
CHEMBL119709 IB-MECA Ki = 1.1 nM 8.96
CHEMBL608755 Ki = 8.0 nM 8.10
CHEMBL611091 Ki = 9.0 nM 8.05
CHEMBL611104 Ki = 10.0 nM 8.00
CHEMBL611095 Ki = 10.0 nM 8.00
CHEMBL610845 Ki = 12.0 nM 7.92
CHEMBL610849 Ki = 14.0 nM 7.85
CHEMBL265587 Ki = 14.8 nM 7.83
CHEMBL610814 Ki = 17.0 nM 7.77
CHEMBL610846 Ki = 19.0 nM 7.72
CHEMBL611089 Ki = 20.0 nM 7.70
CHEMBL610589 Ki = 20.0 nM 7.70
CHEMBL610847 Ki = 22.0 nM 7.66
CHEMBL611090 Ki = 23.0 nM 7.64
CHEMBL610830 Ki = 23.0 nM 7.64
CHEMBL610584 Ki = 23.0 nM 7.64
CHEMBL610837 Ki = 23.0 nM 7.64
CHEMBL610579 Ki = 24.0 nM 7.62
CHEMBL611092 Ki = 24.0 nM 7.62
CHEMBL611099 Ki = 25.0 nM 7.60
CHEMBL610829 Ki = 35.0 nM 7.46
CHEMBL464859 NECA Ki = 34.8 nM 7.46
CHEMBL610580 Ki = 80.0 nM 7.10