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Assay Detail

CHEMBL2328345

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

Binding
Displacement of [3H]CGS21680 from adenosine A2A receptor in rat brain striatal membrane after 60 mins by liquid scintillation counting analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and structure-activity relationships of 2-hydrazinyladenosine derivatives as A(2A) adenosine receptor ligands.
El-Tayeb A, Gollos S.
Bioorg Med Chem (2013) 21 : 436 -447
PubMed 23245803 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.47 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2326828 1 7.92
CHEMBL464859 NECA 1 7.82
CHEMBL2326842 1 7.79
CHEMBL331372 CGS-21680 1 7.75
CHEMBL2326843 1 7.61
CHEMBL1950554 BINODENOSON 3.0 1 7.59
CHEMBL2326829 1 7.27
CHEMBL2326844 1 7.04
CHEMBL2326831 1 6.48
CHEMBL2326840 1 -
CHEMBL2326839 1 -
CHEMBL2326838 1 -
CHEMBL2326837 1 -
CHEMBL2326836 1 -
CHEMBL2326835 1 -
CHEMBL2326834 1 -
CHEMBL2326833 1 -
CHEMBL2326830 1 -
CHEMBL2326841 1 -
CHEMBL2326832 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2326828 Ki = 12.0 nM 7.92
CHEMBL464859 NECA Ki = 15.0 nM 7.82
CHEMBL2326842 Ki = 16.1 nM 7.79
CHEMBL331372 CGS-21680 Ki = 18.0 nM 7.75
CHEMBL2326843 Ki = 24.4 nM 7.61
CHEMBL1950554 BINODENOSON Ki = 25.5 nM 7.59
CHEMBL2326829 Ki = 53.7 nM 7.27
CHEMBL2326844 Ki = 91.7 nM 7.04
CHEMBL2326831 Ki = 329.0 nM 6.48
CHEMBL2326840 Ki > 1000.0 nM -
CHEMBL2326839 Ki > 1000.0 nM -
CHEMBL2326838 Ki > 1000.0 nM -
CHEMBL2326837 Ki > 1000.0 nM -
CHEMBL2326836 Ki > 1000.0 nM -
CHEMBL2326835 Ki > 1000.0 nM -
CHEMBL2326834 Ki > 1000.0 nM -
CHEMBL2326833 Ki > 1000.0 nM -
CHEMBL2326830 Ki > 1000.0 nM -
CHEMBL2326841 Ki > 1000.0 nM -
CHEMBL2326832 Ki > 1000.0 nM -