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Assay Detail

CHEMBL645447

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

Binding
Binding affinity against adenosine A2 receptor in rat striatal membranes using [3H]NECA as radioligand
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Nucleosides and nucleotides. 103. 2-Alkynyladenosines: a novel class of selective adenosine A2 receptor agonists with potent antihypertensive effects.
Matsuda A, Shinozaki M, Yamaguchi T, Homma H, Nomoto R, Miyasaka T, Watanabe Y, Abiru T.
J Med Chem (1992) 35 : 241 -252
PubMed 1732541 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 7.54 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL319387 1 8.55
CHEMBL2113507 1 8.27
CHEMBL2094089 1 8.16
CHEMBL2113510 1 8.12
CHEMBL331372 CGS-21680 1 8.06
CHEMBL608309 1 7.99
CHEMBL2113512 1 7.97
CHEMBL2113496 1 7.92
CHEMBL464859 NECA 1 7.91
CHEMBL2113513 1 7.89
CHEMBL2113503 1 7.69
CHEMBL2113522 1 7.67
CHEMBL2113515 1 7.48
CHEMBL2113511 1 7.47
CHEMBL607728 1 7.42
CHEMBL2113476 1 7.40
CHEMBL2113514 1 7.05
CHEMBL1256672 1 6.97
CHEMBL609784 1 6.82
CHEMBL2113523 1 6.51
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 6.38
CHEMBL2113508 1 6.20
CHEMBL606229 1 -
CHEMBL609783 1 -
CHEMBL612163 1 -
CHEMBL606230 1 -
CHEMBL609199 1 -
CHEMBL315101 1 -
CHEMBL612164 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL319387 Ki = 2.8 nM 8.55
CHEMBL2113507 Ki = 5.4 nM 8.27
CHEMBL2094089 Ki = 6.9 nM 8.16
CHEMBL2113510 Ki = 7.5 nM 8.12
CHEMBL331372 CGS-21680 Ki = 8.8 nM 8.06
CHEMBL608309 Ki = 10.2 nM 7.99
CHEMBL2113512 Ki = 10.6 nM 7.97
CHEMBL2113496 Ki = 12.1 nM 7.92
CHEMBL464859 NECA Ki = 12.4 nM 7.91
CHEMBL2113513 Ki = 12.8 nM 7.89
CHEMBL2113503 Ki = 20.5 nM 7.69
CHEMBL2113522 Ki = 21.2 nM 7.67
CHEMBL2113515 Ki = 32.8 nM 7.48
CHEMBL2113511 Ki = 33.7 nM 7.47
CHEMBL607728 Ki = 37.6 nM 7.42
CHEMBL2113476 Ki = 40.1 nM 7.40
CHEMBL2113514 Ki = 88.1 nM 7.05
CHEMBL1256672 Ki = 107.0 nM 6.97
CHEMBL609784 Ki = 150.0 nM 6.82
CHEMBL2113523 Ki = 307.0 nM 6.51
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 421.0 nM 6.38
CHEMBL2113508 Ki = 630.0 nM 6.20
CHEMBL606229 Ki > 567.0 nM -
CHEMBL609783 Ki > 567.0 nM -
CHEMBL612163 Ki > 567.0 nM -
CHEMBL606230 Ki > 567.0 nM -
CHEMBL609199 Ki > 567.0 nM -
CHEMBL315101 Ki > 567.0 nM -
CHEMBL612164 Ki > 567.0 nM -