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Assay Detail

CHEMBL5163974

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

Binding
Displacement of [3H]SCH5826 from human A2AAR incubated for 60 mins by scintillation counter analysis
ChEMBL ↗
43
Total Activities
43
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 A2a (CHEMBL251) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dual-acting antitumor agents targeting the A<sub>2A</sub> adenosine receptor and histone deacetylases: Design and synthesis of 4-(furan-2-yl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine derivatives.
Zhang J, Luo Z, Duan W, Yang K, Ling L, Yan W, Liu R, Wüthrich K, Jiang H, Xie C, Cheng J.
Eur J Med Chem (2022) 236 : 114326 -114326
PubMed 35390714 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 43 6.86 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL447664 VIPADENANT 2.0 1 9.10
CHEMBL5171906 — — 1 8.14
CHEMBL5201523 — — 1 7.99
CHEMBL5189051 — — 1 7.96
CHEMBL5186576 — — 1 7.91
CHEMBL5188801 — — 1 7.83
CHEMBL5195323 — — 1 7.82
CHEMBL5194232 — — 1 7.60
CHEMBL5196802 — — 1 7.59
CHEMBL5173073 — — 1 7.45
CHEMBL5200632 — — 1 7.29
CHEMBL5179765 — — 1 7.28
CHEMBL5188108 — — 1 7.17
CHEMBL5189321 — — 1 7.14
CHEMBL5179716 — — 1 7.14
CHEMBL5204735 — — 1 7.13
CHEMBL5190722 — — 1 6.97
CHEMBL5193403 — — 1 6.90
CHEMBL5208818 — — 1 6.88
CHEMBL5202005 — — 1 6.85
CHEMBL5205560 — — 1 6.83
CHEMBL5171672 — — 1 6.80
CHEMBL5199428 — — 1 6.79
CHEMBL5169338 — — 1 6.56
CHEMBL5200340 — — 1 6.53
CHEMBL5197839 — — 1 6.52
CHEMBL5169828 — — 1 6.48
CHEMBL5190589 — — 1 6.42
CHEMBL5176483 — — 1 6.36
CHEMBL5202905 — — 1 6.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL447664 VIPADENANT Ki = 0.79 nM 9.10
CHEMBL5171906 — Ki = 7.3 nM 8.14
CHEMBL5201523 — Ki = 10.3 nM 7.99
CHEMBL5189051 — Ki = 10.9 nM 7.96
CHEMBL5186576 — Ki = 12.3 nM 7.91
CHEMBL5188801 — Ki = 14.7 nM 7.83
CHEMBL5195323 — Ki = 15.0 nM 7.82
CHEMBL5194232 — Ki = 25.0 nM 7.60
CHEMBL5196802 — Ki = 25.9 nM 7.59
CHEMBL5173073 — Ki = 35.8 nM 7.45
CHEMBL5200632 — Ki = 50.7 nM 7.29
CHEMBL5179765 — Ki = 52.8 nM 7.28
CHEMBL5188108 — Ki = 68.3 nM 7.17
CHEMBL5189321 — Ki = 72.8 nM 7.14
CHEMBL5179716 — Ki = 72.0 nM 7.14
CHEMBL5204735 — Ki = 74.3 nM 7.13
CHEMBL5190722 — Ki = 107.3 nM 6.97
CHEMBL5193403 — Ki = 124.8 nM 6.90
CHEMBL5208818 — Ki = 130.3 nM 6.88
CHEMBL5202005 — Ki = 140.0 nM 6.85
CHEMBL5205560 — Ki = 147.3 nM 6.83
CHEMBL5171672 — Ki = 159.3 nM 6.80
CHEMBL5199428 — Ki = 163.5 nM 6.79
CHEMBL5169338 — Ki = 276.0 nM 6.56
CHEMBL5200340 — Ki = 294.8 nM 6.53
CHEMBL5197839 — Ki = 301.0 nM 6.52
CHEMBL5169828 — Ki = 334.3 nM 6.48
CHEMBL5190589 — Ki = 378.0 nM 6.42
CHEMBL5176483 — Ki = 435.5 nM 6.36
CHEMBL5202905 — Ki = 585.0 nM 6.23
CHEMBL5205993 — Ki = 617.5 nM 6.21
CHEMBL5207324 — Ki = 777.5 nM 6.11
CHEMBL5201509 — Ki = 862.5 nM 6.06
CHEMBL5209296 — Ki = 862.5 nM 6.06
CHEMBL5203443 — Ki = 974.0 nM 6.01
CHEMBL5194109 — Ki = 1562.5 nM 5.81
CHEMBL5184684 — Ki = 1717.5 nM 5.76
CHEMBL5192939 — Ki = 1827.5 nM 5.74
CHEMBL5170997 — Ki = 2535.0 nM 5.60
CHEMBL5185100 — Ki = 3587.5 nM 5.45
CHEMBL5190098 — Ki > 10000.0 nM -
CHEMBL5171122 — Ki > 10000.0 nM -
CHEMBL5207247 — Ki > 10000.0 nM -