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Assay Detail

CHEMBL644778

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

Binding
Binding affinity against adenosine A2 receptor from rat striatum using [3H]NECA as radioligand.
19
Total Activities
19
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

Nucleosides and nucleotides. 112. 2-(1-Hexyn-1-yl)adenosine-5'-uronamides: a new entry of selective A2 adenosine receptor agonists with potent antihypertensive activity.
Homma H, Watanabe Y, Abiru T, Murayama T, Nomura Y, Matsuda A.
J Med Chem (1992) 35 : 2881 -2890
PubMed 1495019 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.84 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL319387 1 8.62
CHEMBL2113532 1 8.59
CHEMBL2094089 1 8.34
CHEMBL410873 1 8.32
CHEMBL2113531 1 8.28
CHEMBL2113496 1 8.21
CHEMBL331372 CGS-21680 1 8.00
CHEMBL464859 NECA 1 8.00
CHEMBL609211 1 7.96
CHEMBL2113480 1 7.72
CHEMBL609475 1 7.36
CHEMBL1256672 1 7.08
CHEMBL2113481 1 6.77
CHEMBL139835 CYPROTERONE ACETATE 3.0 1 6.47
CHEMBL610635 1 -
CHEMBL608033 1 -
CHEMBL609762 1 -
CHEMBL610345 1 -
CHEMBL611259 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL319387 Ki = 2.4 nM 8.62
CHEMBL2113532 Ki = 2.6 nM 8.59
CHEMBL2094089 Ki = 4.6 nM 8.34
CHEMBL410873 Ki = 4.8 nM 8.32
CHEMBL2113531 Ki = 5.2 nM 8.28
CHEMBL2113496 Ki = 6.1 nM 8.21
CHEMBL331372 CGS-21680 Ki = 10.0 nM 8.00
CHEMBL464859 NECA Ki = 10.0 nM 8.00
CHEMBL609211 Ki = 11.0 nM 7.96
CHEMBL2113480 Ki = 19.0 nM 7.72
CHEMBL609475 Ki = 44.0 nM 7.36
CHEMBL1256672 Ki = 83.0 nM 7.08
CHEMBL2113481 Ki = 169.0 nM 6.77
CHEMBL139835 CYPROTERONE ACETATE Ki = 336.0 nM 6.47
CHEMBL610635 Ki > 181.0 nM -
CHEMBL608033 Ki > 181.0 nM -
CHEMBL609762 Ki > 181.0 nM -
CHEMBL610345 Ki > 181.0 nM -
CHEMBL611259 Ki > 181.0 nM -