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

CHEMBL5099285

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

Binding
Inhibition of CA200645 binding to NanoLuc-fused human adenosine A1 receptor N70 2.65A mutant expressed in HEK293 cells measured at 10 mins by NanoBRET competition binding assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A1 (CHEMBL226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Structure-Activity Relationship Studies of Novel Adenosine A<sub>1</sub> Receptor-Selective Agonists.
Preti B, Suchankova A, Deganutti G, Leuenberger M, Barkan K, Manulak I, Huang X, Carvalho S, Ladds G, Lochner M.
J Med Chem (2022) 65 : 14864 -14890
PubMed 36270633 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.16 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5174052 1 7.00
CHEMBL3771208 1 6.01
CHEMBL5179726 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5174052 Ki = 100.0 nM 7.00
CHEMBL3771208 Ki = 977.24 nM 6.01
CHEMBL5179726 Ki = 3311.31 nM 5.48