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Assay Detail

CHEMBL645780

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

Binding
Ability to displace specific radioligand [125I]AB-MECA binding at human Adenosine A3 receptor expressed in CHO cells
10
Total Activities
10
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

Ring-Constrained (N)-methanocarba nucleosides as adenosine receptor agonists: independent 5'-uronamide and 2'-deoxy modifications.
Lee K, Ravi G, Ji XD, Marquez VE, Jacobson KA.
Bioorg Med Chem Lett (2001) 11 : 1333 -1337
PubMed 11392549 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.22 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27376 1 8.82
CHEMBL280580 1 8.62
CHEMBL283057 1 8.21
CHEMBL286739 1 7.65
CHEMBL27443 1 7.52
CHEMBL26759 1 7.07
CHEMBL27952 1 6.77
CHEMBL28057 1 6.04
CHEMBL27593 1 5.96
CHEMBL27502 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27376 Ki = 1.51 nM 8.82
CHEMBL280580 Ki = 2.39 nM 8.62
CHEMBL283057 Ki = 6.19 nM 8.21
CHEMBL286739 Ki = 22.5 nM 7.65
CHEMBL27443 Ki = 29.9 nM 7.52
CHEMBL26759 Ki = 84.7 nM 7.07
CHEMBL27952 Ki = 170.0 nM 6.77
CHEMBL28057 Ki = 912.0 nM 6.04
CHEMBL27593 Ki = 1090.0 nM 5.96
CHEMBL27502 Ki = 2880.0 nM 5.54