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Assay Detail

CHEMBL639434

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

Binding
Binding affinity against adenosine A1 receptor from rat brain membranes using [3H]cyclohexyladenosine as radioligand.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A1 (CHEMBL318)
Type SINGLE PROTEIN
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 6.84 9.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL139835 CYPROTERONE ACETATE 3.0 1 9.12
CHEMBL464859 NECA 1 8.08
CHEMBL609475 1 7.73
CHEMBL2094089 1 7.19
CHEMBL319387 1 6.99
CHEMBL2113496 1 6.93
CHEMBL2113532 1 6.87
CHEMBL2113531 1 6.66
CHEMBL410873 1 6.56
CHEMBL1256672 1 6.28
CHEMBL331372 CGS-21680 1 5.94
CHEMBL2113480 1 5.90
CHEMBL609211 1 5.75
CHEMBL2113481 1 5.71
CHEMBL609762 1 -
CHEMBL610635 1 -
CHEMBL608033 1 -
CHEMBL610345 1 -
CHEMBL611259 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL139835 CYPROTERONE ACETATE Ki = 0.76 nM 9.12
CHEMBL464859 NECA Ki = 8.3 nM 8.08
CHEMBL609475 Ki = 18.7 nM 7.73
CHEMBL2094089 Ki = 64.0 nM 7.19
CHEMBL319387 Ki = 103.0 nM 6.99
CHEMBL2113496 Ki = 117.0 nM 6.93
CHEMBL2113532 Ki = 136.0 nM 6.87
CHEMBL2113531 Ki = 217.0 nM 6.66
CHEMBL410873 Ki = 276.0 nM 6.56
CHEMBL1256672 Ki = 529.0 nM 6.28
CHEMBL331372 CGS-21680 Ki = 1138.0 nM 5.94
CHEMBL2113480 Ki = 1270.0 nM 5.90
CHEMBL609211 Ki = 1785.0 nM 5.75
CHEMBL2113481 Ki = 1932.0 nM 5.71
CHEMBL609762 Ki > 472.0 nM -
CHEMBL610635 Ki > 472.0 nM -
CHEMBL608033 Ki > 472.0 nM -
CHEMBL610345 Ki > 472.0 nM -
CHEMBL611259 Ki > 472.0 nM -