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Assay Detail

CHEMBL646366

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Binding
Tested for inhibition of adenosine A2 receptor binding to rat brain
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adenosine A2 receptor (CHEMBL2094117)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

The synthesis and biochemical evaluation of new A1 selective adenosine receptor agonists containing 6-hydrazinopurine moieties
Knutsen LJ, Lau J, Sheardown MJ, Thomsen C
Bioorg Med Chem Lett (1993) 3 : 2661 -2666
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 6.04 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL92210 1 7.77
CHEMBL430459 1 7.48
CHEMBL88963 1 6.66
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 6.49
CHEMBL433009 1 6.34
CHEMBL88439 1 6.33
CHEMBL328097 1 6.25
CHEMBL91304 1 6.20
CHEMBL284969 1 6.18
CHEMBL327195 1 6.14
CHEMBL316112 1 5.98
CHEMBL313306 1 5.98
CHEMBL88815 1 5.96
CHEMBL88911 1 5.95
CHEMBL413506 1 5.92
CHEMBL314730 1 5.86
CHEMBL423315 1 5.83
CHEMBL88841 1 5.82
CHEMBL92311 1 5.76
CHEMBL91780 1 5.57
CHEMBL329189 1 5.55
CHEMBL264013 1 5.48
CHEMBL89572 1 5.25
CHEMBL91894 1 4.24
CHEMBL89543 1 -
CHEMBL313806 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL92210 Ki = 17.0 nM 7.77
CHEMBL430459 Ki = 33.0 nM 7.48
CHEMBL88963 Ki = 220.0 nM 6.66
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 321.0 nM 6.49
CHEMBL433009 Ki = 459.0 nM 6.34
CHEMBL88439 Ki = 470.0 nM 6.33
CHEMBL328097 Ki = 564.0 nM 6.25
CHEMBL91304 Ki = 638.0 nM 6.20
CHEMBL284969 Ki = 667.0 nM 6.18
CHEMBL327195 Ki = 720.0 nM 6.14
CHEMBL316112 Ki = 1050.0 nM 5.98
CHEMBL313306 Ki = 1040.0 nM 5.98
CHEMBL88815 Ki = 1100.0 nM 5.96
CHEMBL88911 Ki = 1130.0 nM 5.95
CHEMBL413506 Ki = 1200.0 nM 5.92
CHEMBL314730 Ki = 1380.0 nM 5.86
CHEMBL423315 Ki = 1485.0 nM 5.83
CHEMBL88841 Ki = 1520.0 nM 5.82
CHEMBL92311 Ki = 1733.0 nM 5.76
CHEMBL91780 Ki = 2700.0 nM 5.57
CHEMBL329189 Ki = 2825.0 nM 5.55
CHEMBL264013 Ki = 3320.0 nM 5.48
CHEMBL89572 Ki = 5571.0 nM 5.25
CHEMBL91894 Ki = 57000.0 nM 4.24
CHEMBL89543 Ki > 30000.0 nM -
CHEMBL313806 Ki > 10000.0 nM -