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Assay Detail

CHEMBL4369928

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

Binding
Displacement of [125I]N6-(4-amino-3-iodobenzyl)adenosine-5-N-methyluronamide from mouse A3A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and in Vivo Characterization of A<sub>1</sub> Adenosine Receptor Agonists in the Native Ribose and Conformationally Constrained (N)-Methanocarba Series.
Tosh DK, Rao H, Bitant A, Salmaso V, Mannes P, Lieberman DI, Vaughan KL, Mattison JA, Rothwell AC, Auchampach JA, Ciancetta A, Liu N, Cui Z, Gao ZG, Reitman ML, Gavrilova O, Jacobson KA.
J Med Chem (2019) 62 : 1502 -1522
PubMed 30605331 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 6.37 8.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL331291 1 8.46
CHEMBL464859 NECA 1 7.85
CHEMBL284969 1 7.77
CHEMBL4463802 1 7.53
CHEMBL4471712 1 6.42
CHEMBL1877326 1 6.37
CHEMBL4579650 1 6.35
CHEMBL4556466 1 6.30
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 6.27
CHEMBL4587144 1 6.24
CHEMBL4470080 1 6.21
CHEMBL4468006 1 6.18
CHEMBL4436917 1 6.14
CHEMBL4533718 1 6.05
CHEMBL4436786 1 6.04
CHEMBL4554295 1 6.03
CHEMBL2012686 1 5.97
CHEMBL4522864 1 5.81
CHEMBL4541086 1 5.81
CHEMBL4439013 1 5.68
CHEMBL4562258 1 5.62
CHEMBL4584140 1 5.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL331291 Ki = 3.46 nM 8.46
CHEMBL464859 NECA Ki = 14.1 nM 7.85
CHEMBL284969 Ki = 17.0 nM 7.77
CHEMBL4463802 Ki = 29.5 nM 7.53
CHEMBL4471712 Ki = 385.0 nM 6.42
CHEMBL1877326 Ki = 424.0 nM 6.37
CHEMBL4579650 Ki = 447.0 nM 6.35
CHEMBL4556466 Ki = 503.0 nM 6.30
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 534.0 nM 6.27
CHEMBL4587144 Ki = 574.0 nM 6.24
CHEMBL4470080 Ki = 612.0 nM 6.21
CHEMBL4468006 Ki = 653.0 nM 6.18
CHEMBL4436917 Ki = 718.0 nM 6.14
CHEMBL4533718 Ki = 897.0 nM 6.05
CHEMBL4436786 Ki = 918.0 nM 6.04
CHEMBL4554295 Ki = 934.0 nM 6.03
CHEMBL2012686 Ki = 1060.0 nM 5.97
CHEMBL4522864 Ki = 1560.0 nM 5.81
CHEMBL4541086 Ki = 1560.0 nM 5.81
CHEMBL4439013 Ki = 2110.0 nM 5.68
CHEMBL4562258 Ki = 2410.0 nM 5.62
CHEMBL4584140 Ki = 7440.0 nM 5.13