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Assay Detail

CHEMBL5042666

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

Binding
Displacement of [3H]DPCPX from human A1 adenosine receptor expressed in Flp-In-CHO cells by radioligand competitive binding assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Development and Application of Subtype-Selective Fluorescent Antagonists for the Study of the Human Adenosine A<sub>1</sub> Receptor in Living Cells.
Comeo E, Trinh P, Nguyen AT, Nowell CJ, Kindon ND, Soave M, Stoddart LA, White JM, Hill SJ, Kellam B, Halls ML, May LT, Scammells PJ.
J Med Chem (2021) 64 : 6670 -6695
PubMed 33724031 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.89 9.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5075285 1 9.54
CHEMBL4204703 1 8.77
CHEMBL5086635 1 8.36
CHEMBL5080416 1 8.23
CHEMBL5074153 1 8.11
CHEMBL5080679 1 8.01
CHEMBL5077560 1 7.95
CHEMBL5094274 1 7.89
CHEMBL5090230 1 7.88
CHEMBL5079788 1 7.86
CHEMBL5081778 1 7.83
CHEMBL5090546 1 7.79
CHEMBL5078265 1 7.76
CHEMBL5083466 1 7.69
CHEMBL5083938 1 7.65
CHEMBL5086197 1 6.70
CHEMBL5078024 1 6.07
CHEMBL5075098 1 -
CHEMBL5074915 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5075285 Ki = 0.2884 nM 9.54
CHEMBL4204703 Ki = 1.698 nM 8.77
CHEMBL5086635 Ki = 4.365 nM 8.36
CHEMBL5080416 Ki = 5.888 nM 8.23
CHEMBL5074153 Ki = 7.762 nM 8.11
CHEMBL5080679 Ki = 9.772 nM 8.01
CHEMBL5077560 Ki = 11.22 nM 7.95
CHEMBL5094274 Ki = 12.88 nM 7.89
CHEMBL5090230 Ki = 13.18 nM 7.88
CHEMBL5079788 Ki = 13.8 nM 7.86
CHEMBL5081778 Ki = 14.79 nM 7.83
CHEMBL5090546 Ki = 16.22 nM 7.79
CHEMBL5078265 Ki = 17.38 nM 7.76
CHEMBL5083466 Ki = 20.42 nM 7.69
CHEMBL5083938 Ki = 22.39 nM 7.65
CHEMBL5086197 Ki = 199.53 nM 6.70
CHEMBL5078024 Ki = 851.14 nM 6.07
CHEMBL5075098 Ki > 10000.0 nM -
CHEMBL5074915 Ki > 10000.0 nM -