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Assay Detail

CHEMBL646356

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

Binding
Ability to displace specific radioligand [3H]-CGS- 21680 binding at A2A receptors (rA2A) in rat brain membrane
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A2a (CHEMBL302)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 7 5.66 6.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL280580 1 6.26
CHEMBL417292 1 6.22
CHEMBL27809 1 6.13
CHEMBL27376 1 5.78
CHEMBL284216 1 5.47
CHEMBL27952 1 5.17
CHEMBL28057 1 4.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL280580 Ki = 548.0 nM 6.26
CHEMBL417292 Ki = 601.0 nM 6.22
CHEMBL27809 Ki = 732.0 nM 6.13
CHEMBL27376 Ki = 1660.0 nM 5.78
CHEMBL284216 Ki = 3390.0 nM 5.47
CHEMBL27952 Ki = 6800.0 nM 5.17
CHEMBL28057 Ki = 25400.0 nM 4.59