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Assay Detail

CHEMBL5039183

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Binding
Displacement of [3H]-DPCPX from human A1 receptor expressed in CHO cell membranes measured after 3 hrs by radioligand binding assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Crystal Structure and Subsequent Ligand Design of a Nonriboside Partial Agonist Bound to the Adenosine A<sub>2A</sub> Receptor.
Amelia T, van Veldhoven JPD, Falsini M, Liu R, Heitman LH, van Westen GJP, Segala E, Verdon G, Cheng RKY, Cooke RM, van der Es D, IJzerman AP.
J Med Chem (2021) 64 : 3827 -3842
PubMed 33764785 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.10 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL124345 1 8.52
CHEMBL5093654 1 7.16
CHEMBL5078507 1 7.07
CHEMBL5093743 1 6.95
CHEMBL5091876 1 6.54
CHEMBL5088305 1 6.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL124345 Ki = 3.02 nM 8.52
CHEMBL5093654 Ki = 69.18 nM 7.16
CHEMBL5078507 Ki = 85.11 nM 7.07
CHEMBL5093743 Ki = 112.2 nM 6.95
CHEMBL5091876 Ki = 288.4 nM 6.54
CHEMBL5088305 Ki = 416.87 nM 6.38