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Assay Detail

CHEMBL4731023

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Binding
Binding affinity to human A3AR assessed as inhibitor constant
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Direct Comparison of (N)-Methanocarba and Ribose-Containing 2-Arylalkynyladenosine Derivatives as A Receptor Agonists.
Tosh DK,Salmaso V,Rao H,Campbell R,Bitant A,Gao ZG,Auchampach JA,Jacobson KA
ACS Med Chem Lett (2020) 11 : 1935 -1941
PubMed 33062176 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.95 9.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL574602 1 9.36
CHEMBL3407784 1 9.15
CHEMBL4755127 1 9.12
CHEMBL431733 NAMODENOSON 3.0 1 8.85
CHEMBL119709 IB-MECA 1 8.76
CHEMBL2064657 1 8.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL574602 Ki = 0.44 nM 9.36
CHEMBL3407784 Ki = 0.7 nM 9.15
CHEMBL4755127 Ki = 0.75 nM 9.12
CHEMBL431733 NAMODENOSON Ki = 1.4 nM 8.85
CHEMBL119709 IB-MECA Ki = 1.74 nM 8.76
CHEMBL2064657 Ki = 3.49 nM 8.46