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Assay Detail

CHEMBL648805

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

Binding
Binding affinity against adenosine A2 receptor in rat striatum by using [3H]NECA as a radioligand
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

N6,9-disubstituted adenines: potent, selective antagonists at the A1 adenosine receptor.
Thompson RD, Secunda S, Daly JW, Olsson RA.
J Med Chem (1991) 34 : 2877 -2882
PubMed 1895305 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 4.66 5.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL318453 1 5.17
CHEMBL294590 1 5.09
CHEMBL304009 1 5.06
CHEMBL88788 1 5.03
CHEMBL317398 1 4.96
CHEMBL321753 1 4.96
CHEMBL48278 1 4.96
CHEMBL95332 1 4.89
CHEMBL65976 1 4.82
CHEMBL95936 1 4.82
CHEMBL301574 1 4.77
CHEMBL96014 1 4.75
CHEMBL95617 1 4.72
CHEMBL64239 1 4.64
CHEMBL98779 1 4.51
CHEMBL62756 1 4.42
CHEMBL95913 1 4.41
CHEMBL95897 1 4.34
CHEMBL320370 1 4.33
CHEMBL1202925 1 4.26
CHEMBL321749 1 4.17
CHEMBL319010 1 4.10
CHEMBL1202924 1 4.08
CHEMBL96015 1 -
CHEMBL99407 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL318453 Ki = 6800.0 nM 5.17
CHEMBL294590 Ki = 8200.0 nM 5.09
CHEMBL304009 Ki = 8800.0 nM 5.06
CHEMBL88788 Ki = 9300.0 nM 5.03
CHEMBL317398 Ki = 11000.0 nM 4.96
CHEMBL321753 Ki = 11000.0 nM 4.96
CHEMBL48278 Ki = 11000.0 nM 4.96
CHEMBL95332 Ki = 13000.0 nM 4.89
CHEMBL65976 Ki = 15000.0 nM 4.82
CHEMBL95936 Ki = 15000.0 nM 4.82
CHEMBL301574 Ki = 17000.0 nM 4.77
CHEMBL96014 Ki = 18000.0 nM 4.75
CHEMBL95617 Ki = 19000.0 nM 4.72
CHEMBL64239 Ki = 23000.0 nM 4.64
CHEMBL98779 Ki = 31000.0 nM 4.51
CHEMBL62756 Ki = 38000.0 nM 4.42
CHEMBL95913 Ki = 39000.0 nM 4.41
CHEMBL95897 Ki = 46000.0 nM 4.34
CHEMBL320370 Ki = 47000.0 nM 4.33
CHEMBL1202925 Ki = 55000.0 nM 4.26
CHEMBL321749 Ki = 68000.0 nM 4.17
CHEMBL319010 Ki = 79000.0 nM 4.10
CHEMBL1202924 Ki = 84000.0 nM 4.08
CHEMBL96015 Ki = 111000.0 nM -
CHEMBL99407 Ki = 12000000.0 nM -