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Assay Detail

CHEMBL1102043

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

Binding
Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells after 90 mins by filtration binding assay
19
Total Activities
19
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 A1 (CHEMBL226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent and selective A(2B) adenosine receptor antagonists.
Eastwood P, Gonzalez J, Paredes S, Nueda A, Domenech T, Alberti J, Vidal B.
Bioorg Med Chem Lett (2010) 20 : 1697 -1700
PubMed 20137946 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.61 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1076587 1 7.85
CHEMBL1082005 1 7.60
CHEMBL1081038 1 7.46
CHEMBL1082208 1 7.24
CHEMBL1081812 1 7.09
CHEMBL1082028 1 6.91
CHEMBL1079803 1 6.60
CHEMBL1076562 1 6.54
CHEMBL1079801 1 6.54
CHEMBL1082171 1 6.50
CHEMBL1081041 1 6.47
CHEMBL1081811 1 6.45
CHEMBL1079804 1 6.43
CHEMBL1080676 1 6.20
CHEMBL1080500 1 6.15
CHEMBL1082006 1 6.04
CHEMBL1081971 1 6.03
CHEMBL1081039 1 6.03
CHEMBL375293 1 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1076587 Ki = 14.0 nM 7.85
CHEMBL1082005 Ki = 25.0 nM 7.60
CHEMBL1081038 Ki = 35.0 nM 7.46
CHEMBL1082208 Ki = 58.0 nM 7.24
CHEMBL1081812 Ki = 82.0 nM 7.09
CHEMBL1082028 Ki = 123.0 nM 6.91
CHEMBL1079803 Ki = 250.0 nM 6.60
CHEMBL1076562 Ki = 285.0 nM 6.54
CHEMBL1079801 Ki = 289.0 nM 6.54
CHEMBL1082171 Ki = 320.0 nM 6.50
CHEMBL1081041 Ki = 338.0 nM 6.47
CHEMBL1081811 Ki = 358.0 nM 6.45
CHEMBL1079804 Ki = 374.0 nM 6.43
CHEMBL1080676 Ki = 635.0 nM 6.20
CHEMBL1080500 Ki = 702.0 nM 6.15
CHEMBL1082006 Ki = 914.0 nM 6.04
CHEMBL1081971 Ki = 931.0 nM 6.03
CHEMBL1081039 Ki = 940.0 nM 6.03
CHEMBL375293 Ki = 2821.0 nM 5.55