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Assay Detail

CHEMBL646487

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

Binding
Binding to Adenosine A2 receptor was measured in ADA-pretreated rat striatal membranes using [3H]-CGS- 21680
15
Total Activities
15
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

2-(Arylalkylamino)adenosin-5'-uronamides: a new class of highly selective adenosine A2 receptor ligands.
Hutchison AJ, Williams M, de Jesus R, Yokoyama R, Oei HH, Ghai GR, Webb RL, Zoganas HC, Stone GA, Jarvis MF.
J Med Chem (1990) 33 : 1919 -1924
PubMed 2362269 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.42 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL57706 1 8.12
CHEMBL2374466 1 8.11
CHEMBL2374468 1 8.05
CHEMBL464859 NECA 1 8.05
CHEMBL2042298 1 8.01
CHEMBL2374465 1 7.85
CHEMBL331372 CGS-21680 1 7.72
CHEMBL60860 1 7.38
CHEMBL2374469 1 7.35
CHEMBL1256672 1 7.15
CHEMBL2374463 1 7.15
CHEMBL519809 1 7.15
CHEMBL2374467 1 7.11
CHEMBL139835 CYPROTERONE ACETATE 3.0 1 6.20
CHEMBL2374464 1 5.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL57706 Ki = 7.5 nM 8.12
CHEMBL2374466 Ki = 7.7 nM 8.11
CHEMBL2374468 Ki = 9.0 nM 8.05
CHEMBL464859 NECA Ki = 9.0 nM 8.05
CHEMBL2042298 Ki = 9.7 nM 8.01
CHEMBL2374465 Ki = 14.0 nM 7.85
CHEMBL331372 CGS-21680 Ki = 19.0 nM 7.72
CHEMBL60860 Ki = 42.0 nM 7.38
CHEMBL2374469 Ki = 45.0 nM 7.35
CHEMBL1256672 Ki = 71.0 nM 7.15
CHEMBL2374463 Ki = 71.0 nM 7.15
CHEMBL519809 Ki = 71.0 nM 7.15
CHEMBL2374467 Ki = 77.0 nM 7.11
CHEMBL139835 CYPROTERONE ACETATE Ki = 636.0 nM 6.20
CHEMBL2374464 Ki = 1130.0 nM 5.95