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Assay Detail

CHEMBL3749019

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

Binding
Displacement of [125I]N6-(4-amino-3-iodobenzyl)adenosine-5'-N-methyl-uronamide from human adenosine A3 receptor stably expressed in CHO cell membrane by radioligand binding assay
23
Total Activities
23
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

Transmembrane domain-containing protein TMIGD3 (CHEMBL3712907)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Design, Synthesis by Click Chemistry and in Vivo Activity of Highly Selective A3 Adenosine Receptor Agonists.
Tosh DK, Paoletta S, Chen Z, Crane S, Lloyd J, Gao ZG, Gizewski ET, Auchampach JA, Salvemini D, Jacobson KA.
Medchemcomm (2015) 6 : 555 -563
PubMed 26236460 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 8.84 9.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3747303 1 9.27
CHEMBL3746778 1 9.24
CHEMBL3746260 1 9.16
CHEMBL3612943 1 9.14
CHEMBL3747209 1 9.07
CHEMBL3747005 1 9.07
CHEMBL3746512 1 9.04
CHEMBL3746774 1 9.02
CHEMBL3747276 1 9.02
CHEMBL3746358 1 9.02
CHEMBL3746487 1 8.97
CHEMBL3747457 1 8.97
CHEMBL3612944 1 8.91
CHEMBL3747461 1 8.91
CHEMBL3745837 1 8.90
CHEMBL3746890 1 8.81
CHEMBL3747756 1 8.73
CHEMBL3745807 1 8.67
CHEMBL3747321 1 8.66
CHEMBL3747670 1 8.46
CHEMBL3746784 1 8.18
CHEMBL3745851 1 8.15
CHEMBL3746886 1 8.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3747303 Ki = 0.54 nM 9.27
CHEMBL3746778 Ki = 0.58 nM 9.24
CHEMBL3746260 Ki = 0.69 nM 9.16
CHEMBL3612943 Ki = 0.73 nM 9.14
CHEMBL3747209 Ki = 0.85 nM 9.07
CHEMBL3747005 Ki = 0.85 nM 9.07
CHEMBL3746512 Ki = 0.91 nM 9.04
CHEMBL3746774 Ki = 0.95 nM 9.02
CHEMBL3747276 Ki = 0.96 nM 9.02
CHEMBL3746358 Ki = 0.96 nM 9.02
CHEMBL3746487 Ki = 1.08 nM 8.97
CHEMBL3747457 Ki = 1.06 nM 8.97
CHEMBL3612944 Ki = 1.22 nM 8.91
CHEMBL3747461 Ki = 1.22 nM 8.91
CHEMBL3745837 Ki = 1.25 nM 8.90
CHEMBL3746890 Ki = 1.53 nM 8.81
CHEMBL3747756 Ki = 1.84 nM 8.73
CHEMBL3745807 Ki = 2.16 nM 8.67
CHEMBL3747321 Ki = 2.21 nM 8.66
CHEMBL3747670 Ki = 3.48 nM 8.46
CHEMBL3746784 Ki = 6.66 nM 8.18
CHEMBL3745851 Ki = 7.05 nM 8.15
CHEMBL3746886 Ki = 9.02 nM 8.04