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Assay Detail

CHEMBL3267346

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

Binding
Inhibition of human recombinant adenosine receptor A2b
ChEMBL ↗
54
Total Activities
53
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 A2b (CHEMBL255) ↗
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 54 6.22 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL16687 CGS-15943 — 1 7.36
CHEMBL113142 ZM-241385 — 1 7.30
CHEMBL447664 VIPADENANT 2.0 1 7.20
CHEMBL261203 — — 1 6.95
CHEMBL259832 — — 1 6.85
CHEMBL197669 ST1535 1.0 1 6.45
CHEMBL564473 — — 1 6.34
CHEMBL2105747 TOZADENANT 3.0 1 6.16
CHEMBL407307 — — 1 6.06
CHEMBL17127 SCH-58261 — 1 5.96
CHEMBL431770 ISTRADEFYLLINE 4.0 1 5.75
CHEMBL413079 — — 1 5.54
CHEMBL609578 — — 1 5.50
CHEMBL411329 (R,S)-MEFLOQUINE — 1 5.15
CHEMBL113 CAFFEINE 4.0 1 4.69
CHEMBL3222062 — — 1 -
CHEMBL3222061 — — 1 -
CHEMBL3222055 — — 1 -
CHEMBL1095172 — — 1 -
CHEMBL1095488 — — 1 -
CHEMBL1087189 — — 1 -
CHEMBL1095999 — — 1 -
CHEMBL1370747 — — 1 -
CHEMBL184309 — — 1 -
CHEMBL174628 — — 1 -
CHEMBL426738 — — 1 -
CHEMBL183181 — — 1 -
CHEMBL2165804 — — 1 -
CHEMBL2398486 — — 1 -
CHEMBL2398482 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL16687 CGS-15943 Ki = 44.0 nM 7.36
CHEMBL113142 ZM-241385 Ki = 50.0 nM 7.30
CHEMBL447664 VIPADENANT Ki = 63.0 nM 7.20
CHEMBL261203 — Ki = 112.0 nM 6.95
CHEMBL259832 — Ki = 141.0 nM 6.85
CHEMBL197669 ST1535 Ki = 352.0 nM 6.45
CHEMBL564473 — Ki = 460.0 nM 6.34
CHEMBL2105747 TOZADENANT Ki = 700.0 nM 6.16
CHEMBL407307 — Ki = 865.0 nM 6.06
CHEMBL17127 SCH-58261 Ki = 1110.0 nM 5.96
CHEMBL431770 ISTRADEFYLLINE Ki = 1800.0 nM 5.75
CHEMBL413079 — Ki = 2900.0 nM 5.54
CHEMBL609578 — Ki = 3185.0 nM 5.50
CHEMBL411329 (R,S)-MEFLOQUINE Ki = 7072.0 nM 5.15
CHEMBL113 CAFFEINE Ki = 20500.0 nM 4.69
CHEMBL487553 — Ki - — -
CHEMBL3260727 — Ki - — -
CHEMBL1762513 — Ki - — -
CHEMBL1355736 THEOPHYLLINE Ki - — -
CHEMBL25964 — Ki - — -
CHEMBL520782 — Ki - — -
CHEMBL240624 PRELADENANT Ki - — -
CHEMBL240624 PRELADENANT Ki > 1700.0 nM -
CHEMBL395472 — Ki - — -
CHEMBL246675 — Ki - — -
CHEMBL513364 — Ki - — -
CHEMBL482329 — Ki - — -
CHEMBL598251 — Ki - — -
CHEMBL1762515 — Ki - — -
CHEMBL3260725 — Ki - — -
CHEMBL3260726 — Ki - — -
CHEMBL2024119 — Ki - — -
CHEMBL1095999 — Ki - — -
CHEMBL2398482 — Ki - — -
CHEMBL183181 — Ki - — -
CHEMBL426738 — Ki - — -
CHEMBL174628 — Ki - — -
CHEMBL184309 — Ki - — -
CHEMBL2165804 — Ki - — -
CHEMBL2398486 — Ki - — -
CHEMBL1370747 — Ki - — -
CHEMBL401895 — Ki - — -
CHEMBL1087189 — Ki - — -
CHEMBL1095488 — Ki - — -
CHEMBL1095172 — Ki - — -
CHEMBL3222055 — Ki - — -
CHEMBL3222061 — Ki - — -
CHEMBL3222062 — Ki - — -
CHEMBL401321 — Ki - — -
CHEMBL271202 — Ki - — -