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Assay Detail

CHEMBL3267350

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

Binding
Inhibition of human recombinant adenosine A3 receptor
53
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Adenosine A2A receptor as a drug discovery target.
de Lera Ruiz M, Lim YH, Zheng J.
J Med Chem (2014) 57 : 3623 -3650
PubMed 24164628 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 53 6.00 7.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL16687 CGS-15943 1 7.02
CHEMBL609578 1 6.44
CHEMBL407307 1 6.32
CHEMBL447664 VIPADENANT 2.0 1 6.00
CHEMBL17127 SCH-58261 1 5.92
CHEMBL261203 1 5.83
CHEMBL2105747 TOZADENANT 3.0 1 5.80
CHEMBL564473 1 5.76
CHEMBL259832 1 5.71
CHEMBL411329 (R,S)-MEFLOQUINE 1 5.16
CHEMBL1095999 1 -
CHEMBL1087189 1 -
CHEMBL1095488 1 -
CHEMBL1095172 1 -
CHEMBL3222055 1 -
CHEMBL3222061 1 -
CHEMBL3222062 1 -
CHEMBL401321 1 -
CHEMBL271202 1 -
CHEMBL401895 1 -
CHEMBL2165804 1 -
CHEMBL3260728 1 -
CHEMBL184309 1 -
CHEMBL174628 1 -
CHEMBL426738 1 -
CHEMBL183181 1 -
CHEMBL197669 ST1535 1.0 1 -
CHEMBL598251 1 -
CHEMBL2398486 1 -
CHEMBL2398482 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL16687 CGS-15943 Ki = 95.0 nM 7.02
CHEMBL609578 Ki = 366.0 nM 6.44
CHEMBL407307 Ki = 476.0 nM 6.32
CHEMBL447664 VIPADENANT Ki = 1005.0 nM 6.00
CHEMBL17127 SCH-58261 Ki = 1200.0 nM 5.92
CHEMBL261203 Ki = 1472.0 nM 5.83
CHEMBL2105747 TOZADENANT Ki = 1570.0 nM 5.80
CHEMBL564473 Ki = 1740.0 nM 5.76
CHEMBL259832 Ki = 1931.0 nM 5.71
CHEMBL411329 (R,S)-MEFLOQUINE Ki = 6941.0 nM 5.16
CHEMBL395472 Ki - -
CHEMBL240624 PRELADENANT Ki > 1000.0 nM -
CHEMBL240624 PRELADENANT Ki - -
CHEMBL520782 Ki - -
CHEMBL113142 ZM-241385 Ki > 10000.0 nM -
CHEMBL431770 ISTRADEFYLLINE Ki > 3000.0 nM -
CHEMBL1762515 Ki - -
CHEMBL487553 Ki - -
CHEMBL3260728 Ki - -
CHEMBL401895 Ki - -
CHEMBL246675 Ki - -
CHEMBL513364 Ki - -
CHEMBL482329 Ki - -
CHEMBL1762513 Ki - -
CHEMBL3260732 Ki - -
CHEMBL3260725 Ki - -
CHEMBL3260726 Ki - -
CHEMBL1370747 Ki - -
CHEMBL2024119 Ki - -
CHEMBL1355736 THEOPHYLLINE Ki - -
CHEMBL2398486 Ki - -
CHEMBL197669 ST1535 Ki > 10000.0 nM -
CHEMBL2398482 Ki - -
CHEMBL1085997 Ki - -
CHEMBL183181 Ki - -
CHEMBL426738 Ki - -
CHEMBL174628 Ki - -
CHEMBL184309 Ki - -
CHEMBL598251 Ki - -
CHEMBL3260727 Ki - -
CHEMBL271202 Ki - -
CHEMBL2165804 Ki > 557.0 nM -
CHEMBL1095999 Ki - -
CHEMBL1087189 Ki - -
CHEMBL1095488 Ki - -
CHEMBL1095172 Ki - -
CHEMBL3222055 Ki - -
CHEMBL3222061 Ki - -
CHEMBL3222062 Ki - -
CHEMBL401321 Ki - -