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Assay Detail

CHEMBL2187069

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

Binding
Displacement of [125I]I-AB-MECA from human rat adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counter
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A3 (CHEMBL3360)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications.
Baraldi PG, Preti D, Borea PA, Varani K.
J Med Chem (2012) 55 : 5676 -5703
PubMed 22468757 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.06 9.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL431733 NAMODENOSON 3.0 1 9.48
CHEMBL175543 1 9.00
CHEMBL119709 IB-MECA 1 8.96
CHEMBL2181976 1 8.80
CHEMBL138746 1 6.64
CHEMBL193421 1 6.40
CHEMBL193692 1 6.27
CHEMBL108705 1 6.09
CHEMBL265096 1 5.42
CHEMBL128929 1 5.38
CHEMBL89093 1 5.26
CHEMBL2181975 1 -
CHEMBL2181972 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL431733 NAMODENOSON Ki = 0.33 nM 9.48
CHEMBL175543 Ki = 1.0 nM 9.00
CHEMBL119709 IB-MECA Ki = 1.1 nM 8.96
CHEMBL2181976 Ki = 1.6 nM 8.80
CHEMBL138746 Ki = 229.0 nM 6.64
CHEMBL193421 Ki = 399.0 nM 6.40
CHEMBL193692 Ki = 538.0 nM 6.27
CHEMBL108705 Ki = 814.0 nM 6.09
CHEMBL265096 Ki = 3850.0 nM 5.42
CHEMBL128929 Ki = 4200.0 nM 5.38
CHEMBL89093 Ki = 5500.0 nM 5.26
CHEMBL2181975 Ki > 10000.0 nM -
CHEMBL2181972 Ki > 10000.0 nM -