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Assay Detail

CHEMBL3750699

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

Binding
Displacement of CA200645 from human adenosine A3 receptor expressed in CHO CRE-SPAP cells incubated for 1 hr by fluorescence analysis
18
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Transmembrane domain-containing protein TMIGD3 (CHEMBL3712907)
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 18 6.31 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3745868 2 7.47
CHEMBL3747370 2 6.98
CHEMBL3746510 2 6.96
CHEMBL3747100 1 6.86
CHEMBL1316867 1 6.48
CHEMBL2006198 1 6.42
CHEMBL3745825 1 6.40
CHEMBL3745803 1 6.26
CHEMBL3746858 1 5.74
CHEMBL1417979 1 5.70
CHEMBL3747257 1 5.66
CHEMBL1536674 1 5.64
CHEMBL3746686 1 5.62
CHEMBL3746209 1 5.31
CHEMBL6215 1 4.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3745868 Ki = 33.88 nM 7.47
CHEMBL3745868 Ki = 40.0 nM 7.40
CHEMBL3747370 Ki = 104.71 nM 6.98
CHEMBL3746510 Ki = 109.65 nM 6.96
CHEMBL3746510 Ki = 120.0 nM 6.92
CHEMBL3747370 Ki = 120.0 nM 6.92
CHEMBL3747100 Ki = 138.04 nM 6.86
CHEMBL1316867 Ki = 331.13 nM 6.48
CHEMBL2006198 Ki = 380.19 nM 6.42
CHEMBL3745825 Ki = 398.11 nM 6.40
CHEMBL3745803 Ki = 549.54 nM 6.26
CHEMBL3746858 Ki = 1819.7 nM 5.74
CHEMBL1417979 Ki = 1995.26 nM 5.70
CHEMBL3747257 Ki = 2187.76 nM 5.66
CHEMBL1536674 Ki = 2290.87 nM 5.64
CHEMBL3746686 Ki = 2398.83 nM 5.62
CHEMBL3746209 Ki = 4897.79 nM 5.31
CHEMBL6215 Ki = 13489.63 nM 4.87