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Assay Detail

CHEMBL649866

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

Binding
Inhibition of [3H]NECA binding to adenosine A2 receptor from rat striatal membranes
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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. 107. 2-(cycloalkylalkynyl)adenosines: adenosine A2 receptor agonists with potent antihypertensive effects.
Abiru T, Miyashita T, Watanabe Y, Yamaguchi T, Machida H, Matsuda A.
J Med Chem (1992) 35 : 2253 -2260
PubMed 1613750 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 8.17 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2113497 1 9.05
CHEMBL2113501 1 8.96
CHEMBL608594 1 8.74
CHEMBL2092941 1 8.72
CHEMBL2113498 1 8.72
CHEMBL608299 1 8.70
CHEMBL2113499 1 8.64
CHEMBL319387 1 8.55
CHEMBL608899 1 8.48
CHEMBL610362 1 8.47
CHEMBL610651 1 8.19
CHEMBL2094089 1 8.16
CHEMBL2113496 1 8.10
CHEMBL331372 CGS-21680 1 8.06
CHEMBL609493 1 8.00
CHEMBL2113504 1 7.92
CHEMBL2113506 1 7.75
CHEMBL2113505 1 7.72
CHEMBL2113503 1 7.70
CHEMBL608298 1 7.58
CHEMBL2113500 1 7.43
CHEMBL612161 1 7.34
CHEMBL375190 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2113497 Ki = 0.9 nM 9.05
CHEMBL2113501 Ki = 1.1 nM 8.96
CHEMBL608594 Ki = 1.8 nM 8.74
CHEMBL2092941 Ki = 1.9 nM 8.72
CHEMBL2113498 Ki = 1.9 nM 8.72
CHEMBL608299 Ki = 2.0 nM 8.70
CHEMBL2113499 Ki = 2.3 nM 8.64
CHEMBL319387 Ki = 2.8 nM 8.55
CHEMBL608899 Ki = 3.3 nM 8.48
CHEMBL610362 Ki = 3.4 nM 8.47
CHEMBL610651 Ki = 6.5 nM 8.19
CHEMBL2094089 Ki = 6.9 nM 8.16
CHEMBL2113496 Ki = 7.9 nM 8.10
CHEMBL331372 CGS-21680 Ki = 8.8 nM 8.06
CHEMBL609493 Ki = 10.0 nM 8.00
CHEMBL2113504 Ki = 12.0 nM 7.92
CHEMBL2113506 Ki = 18.0 nM 7.75
CHEMBL2113505 Ki = 19.0 nM 7.72
CHEMBL2113503 Ki = 20.0 nM 7.70
CHEMBL608298 Ki = 26.0 nM 7.58
CHEMBL2113500 Ki = 37.0 nM 7.43
CHEMBL612161 Ki = 46.0 nM 7.34
CHEMBL375190 Ki = 109.0 nM 6.96