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Assay Detail

CHEMBL860157

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

Binding
Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells
29
Total Activities
29
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 Expert

Target

Adenosine receptor A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1,2,4-Triazolo[1,5-a]quinoxaline as a versatile tool for the design of selective human A3 adenosine receptor antagonists: synthesis, biological evaluation, and molecular modeling studies of 2-(hetero)aryl- and 2-carboxy-substituted derivatives.
Catarzi D, Colotta V, Varano F, Lenzi O, Filacchioni G, Trincavelli L, Martini C, Montopoli C, Moro S.
J Med Chem (2005) 48 : 7932 -7945
PubMed 16335918 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 7.02 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL328437 1 8.70
CHEMBL99178 1 8.68
CHEMBL197376 1 8.60
CHEMBL200479 1 8.54
CHEMBL316824 1 8.22
CHEMBL110165 1 7.60
CHEMBL98678 1 7.59
CHEMBL178863 1 7.55
CHEMBL330399 1 7.48
CHEMBL325715 1 7.29
CHEMBL86164 1 7.15
CHEMBL327853 1 7.11
CHEMBL334286 1 7.09
CHEMBL200835 1 7.04
CHEMBL9128 1 6.97
CHEMBL197325 1 6.96
CHEMBL97286 1 6.90
CHEMBL198574 1 6.79
CHEMBL94830 1 6.59
CHEMBL371697 1 6.51
CHEMBL83919 1 6.47
CHEMBL310544 1 6.45
CHEMBL197333 1 6.40
CHEMBL116737 1 6.38
CHEMBL83855 1 6.25
CHEMBL8907 1 6.17
CHEMBL179109 1 6.09
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 5.89
CHEMBL1355736 THEOPHYLLINE 4.0 1 4.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL328437 Ki = 2.0 nM 8.70
CHEMBL99178 Ki = 2.1 nM 8.68
CHEMBL197376 Ki = 2.5 nM 8.60
CHEMBL200479 Ki = 2.9 nM 8.54
CHEMBL316824 Ki = 6.0 nM 8.22
CHEMBL110165 Ki = 25.0 nM 7.60
CHEMBL98678 Ki = 25.8 nM 7.59
CHEMBL178863 Ki = 28.2 nM 7.55
CHEMBL330399 Ki = 33.0 nM 7.48
CHEMBL325715 Ki = 51.6 nM 7.29
CHEMBL86164 Ki = 70.8 nM 7.15
CHEMBL327853 Ki = 78.0 nM 7.11
CHEMBL334286 Ki = 82.0 nM 7.09
CHEMBL200835 Ki = 91.4 nM 7.04
CHEMBL9128 Ki = 108.0 nM 6.97
CHEMBL197325 Ki = 111.0 nM 6.96
CHEMBL97286 Ki = 126.0 nM 6.90
CHEMBL198574 Ki = 163.0 nM 6.79
CHEMBL94830 Ki = 257.0 nM 6.59
CHEMBL371697 Ki = 308.0 nM 6.51
CHEMBL83919 Ki = 340.0 nM 6.47
CHEMBL310544 Ki = 354.0 nM 6.45
CHEMBL197333 Ki = 396.0 nM 6.40
CHEMBL116737 Ki = 420.0 nM 6.38
CHEMBL83855 Ki = 557.0 nM 6.25
CHEMBL8907 Ki = 673.0 nM 6.17
CHEMBL179109 Ki = 820.0 nM 6.09
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 1300.0 nM 5.89
CHEMBL1355736 THEOPHYLLINE Ki = 86000.0 nM 4.07