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Assay Detail

CHEMBL3750700

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

Binding
Displacement of CA200645 from human adenosine A1 receptor expressed in CHO cells incubated for 1 hr by fluorescence analysis
15
Total Activities
15
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

Fragment-Based Discovery of Subtype-Selective Adenosine Receptor Ligands from Homology Models.
Ranganathan A, Stoddart LA, Hill SJ, Carlsson J.
J Med Chem (2015) 58 : 9578 -9590
PubMed 26592528 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 5.11 6.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3747100 1 6.46
CHEMBL3745825 1 5.71
CHEMBL2006198 1 5.55
CHEMBL3747370 1 5.53
CHEMBL3746510 1 5.51
CHEMBL3746686 1 5.50
CHEMBL3745868 1 5.43
CHEMBL1316867 1 5.21
CHEMBL3746209 1 4.91
CHEMBL1417979 1 4.64
CHEMBL3747257 1 4.53
CHEMBL3745803 1 4.25
CHEMBL3746858 1 4.21
CHEMBL6215 1 4.12
CHEMBL1536674 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3747100 Ki = 346.74 nM 6.46
CHEMBL3745825 Ki = 1949.84 nM 5.71
CHEMBL2006198 Ki = 2818.38 nM 5.55
CHEMBL3747370 Ki = 2951.21 nM 5.53
CHEMBL3746510 Ki = 3090.3 nM 5.51
CHEMBL3746686 Ki = 3162.28 nM 5.50
CHEMBL3745868 Ki = 3715.35 nM 5.43
CHEMBL1316867 Ki = 6165.95 nM 5.21
CHEMBL3746209 Ki = 12302.69 nM 4.91
CHEMBL1417979 Ki = 22908.68 nM 4.64
CHEMBL3747257 Ki = 29512.09 nM 4.53
CHEMBL3745803 Ki = 56234.13 nM 4.25
CHEMBL3746858 Ki = 61659.5 nM 4.21
CHEMBL6215 Ki = 75857.76 nM 4.12
CHEMBL1536674 Ki < 100000.0 nM -