Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1769839

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

Binding
Displacement of [125I]AB-MECA from human cloned adenosine A3 receptor expressed in CHO cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The identification of the 2-phenylphthalazin-1(2H)-one scaffold as a new decorable core skeleton for the design of potent and selective human A3 adenosine receptor antagonists.
Poli D, Catarzi D, Colotta V, Varano F, Filacchioni G, Daniele S, Trincavelli L, Martini C, Paoletta S, Moro S.
J Med Chem (2011) 54 : 2102 -2113
PubMed 21401121 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.21 9.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1766358 1 9.11
CHEMBL1766354 1 8.05
CHEMBL1766353 1 8.01
CHEMBL1766359 1 7.53
CHEMBL1766352 1 7.22
CHEMBL1766271 1 6.75
CHEMBL1766360 1 6.56
CHEMBL16254 1 6.56
CHEMBL278197 1 6.31
CHEMBL1766267 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1766358 Ki = 0.776 nM 9.11
CHEMBL1766354 Ki = 8.9 nM 8.05
CHEMBL1766353 Ki = 9.75 nM 8.01
CHEMBL1766359 Ki = 29.6 nM 7.53
CHEMBL1766352 Ki = 60.6 nM 7.22
CHEMBL1766271 Ki = 178.4 nM 6.75
CHEMBL1766360 Ki = 274.2 nM 6.56
CHEMBL16254 Ki = 276.0 nM 6.56
CHEMBL278197 Ki = 490.0 nM 6.31
CHEMBL1766267 Ki = 1100.0 nM 5.96