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Assay Detail

CHEMBL645784

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

Binding
Affinity for human Adenosine A3 receptor expressed in CHO cell
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.
Gao ZG, Kim SK, Biadatti T, Chen W, Lee K, Barak D, Kim SG, Johnson CR, Jacobson KA.
J Med Chem (2002) 45 : 4471 -4484
PubMed 12238926 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 7.76 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL139417 1 8.89
CHEMBL431733 NAMODENOSON 3.0 1 8.85
CHEMBL369744 1 8.82
CHEMBL119709 IB-MECA 1 8.74
CHEMBL307199 1 8.74
CHEMBL342873 1 8.72
CHEMBL133387 1 8.68
CHEMBL345076 1 8.47
CHEMBL66393 1 8.24
CHEMBL139000 (R)-PIA 1 8.06
CHEMBL138781 1 8.04
CHEMBL344187 1 7.53
CHEMBL464859 NECA 1 7.46
CHEMBL284969 1 7.42
CHEMBL420705 (S)-PIA 1 7.17
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 7.14
CHEMBL285819 1 7.06
CHEMBL290077 1 7.00
CHEMBL141792 1 6.94
CHEMBL337602 1 6.45
CHEMBL342926 1 6.24
CHEMBL138746 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL139417 Ki = 1.3 nM 8.89
CHEMBL431733 NAMODENOSON Ki = 1.4 nM 8.85
CHEMBL369744 Ki = 1.5 nM 8.82
CHEMBL119709 IB-MECA Ki = 1.8 nM 8.74
CHEMBL307199 Ki = 1.8 nM 8.74
CHEMBL342873 Ki = 1.9 nM 8.72
CHEMBL133387 Ki = 2.1 nM 8.68
CHEMBL345076 Ki = 3.4 nM 8.47
CHEMBL66393 Ki = 5.8 nM 8.24
CHEMBL139000 (R)-PIA Ki = 8.7 nM 8.06
CHEMBL138781 Ki = 9.2 nM 8.04
CHEMBL344187 Ki = 29.3 nM 7.53
CHEMBL464859 NECA Ki = 35.0 nM 7.46
CHEMBL284969 Ki = 38.0 nM 7.42
CHEMBL420705 (S)-PIA Ki = 68.0 nM 7.17
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 72.0 nM 7.14
CHEMBL285819 Ki = 87.0 nM 7.06
CHEMBL290077 Ki = 99.0 nM 7.00
CHEMBL141792 Ki = 114.0 nM 6.94
CHEMBL337602 Ki = 353.0 nM 6.45
CHEMBL342926 Ki = 572.0 nM 6.24
CHEMBL138746 Ki = 816.0 nM 6.09