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Assay Detail

CHEMBL644772

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

Binding
Binding affinity against A2 adenosine receptors of the central nervous system
20
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

Analogues of 1,3-dipropyl-8-phenylxanthine: enhancement of selectivity at A1-adenosine receptors by aryl substituents.
Daly JW, Padgett WL, Shamim MT.
J Med Chem (1986) 29 : 1520 -1524
PubMed 3016270 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 6.82 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL36783 1 7.92
CHEMBL415971 1 7.89
CHEMBL32598 1 7.55
CHEMBL27155 1 7.30
CHEMBL156627 2 7.26
CHEMBL347687 1 7.02
CHEMBL39770 1 7.00
CHEMBL423239 1 6.96
CHEMBL290589 1 6.94
CHEMBL36702 1 6.85
CHEMBL36740 1 6.68
CHEMBL290076 1 6.54
CHEMBL158507 1 6.52
CHEMBL156863 1 6.40
CHEMBL418333 1 6.15
CHEMBL350469 1 6.01
CHEMBL273671 1 6.00
CHEMBL36867 1 5.46
CHEMBL290643 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL36783 Ki = 12.0 nM 7.92
CHEMBL415971 Ki = 13.0 nM 7.89
CHEMBL32598 Ki = 28.0 nM 7.55
CHEMBL27155 Ki = 50.0 nM 7.30
CHEMBL156627 Ki = 55.0 nM 7.26
CHEMBL156627 Ki = 72.0 nM 7.14
CHEMBL347687 Ki = 95.0 nM 7.02
CHEMBL39770 Ki = 100.0 nM 7.00
CHEMBL423239 Ki = 110.0 nM 6.96
CHEMBL290589 Ki = 115.0 nM 6.94
CHEMBL36702 Ki = 140.0 nM 6.85
CHEMBL36740 Ki = 210.0 nM 6.68
CHEMBL290076 Ki = 290.0 nM 6.54
CHEMBL158507 Ki = 300.0 nM 6.52
CHEMBL156863 Ki = 400.0 nM 6.40
CHEMBL418333 Ki = 710.0 nM 6.15
CHEMBL350469 Ki = 980.0 nM 6.01
CHEMBL273671 Ki = 1000.0 nM 6.00
CHEMBL36867 Ki = 3500.0 nM 5.46
CHEMBL290643 Ki > 3000.0 nM -