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Assay Detail

CHEMBL649107

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Binding
Ability to displace specific radioligand [3H]R-PIA binding at Adenosine A1 receptor in rat brain membrane
15
Total Activities
15
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 A1 (CHEMBL318)
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 15 6.56 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27952 1 8.30
CHEMBL284216 1 8.06
CHEMBL27443 1 7.50
CHEMBL280580 1 7.28
CHEMBL417292 1 7.16
CHEMBL27376 1 7.08
CHEMBL27809 1 6.85
CHEMBL26759 1 6.56
CHEMBL283057 1 6.09
CHEMBL286739 1 6.05
CHEMBL27009 1 5.83
CHEMBL287321 1 5.78
CHEMBL27593 1 5.44
CHEMBL27502 1 5.29
CHEMBL28057 1 5.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27952 Ki = 5.06 nM 8.30
CHEMBL284216 Ki = 8.76 nM 8.06
CHEMBL27443 Ki = 31.8 nM 7.50
CHEMBL280580 Ki = 52.7 nM 7.28
CHEMBL417292 Ki = 69.2 nM 7.16
CHEMBL27376 Ki = 83.9 nM 7.08
CHEMBL27809 Ki = 141.0 nM 6.85
CHEMBL26759 Ki = 273.0 nM 6.56
CHEMBL283057 Ki = 805.0 nM 6.09
CHEMBL286739 Ki = 884.0 nM 6.05
CHEMBL27009 Ki = 1470.0 nM 5.83
CHEMBL287321 Ki = 1680.0 nM 5.78
CHEMBL27593 Ki = 3600.0 nM 5.44
CHEMBL27502 Ki = 5110.0 nM 5.29
CHEMBL28057 Ki = 8730.0 nM 5.06