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Assay Detail

CHEMBL3090423

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

Binding
Displacement of [3H]NECA from human recombinant adenosine A2A receptor expressed in CHO cells
17
Total Activities
17
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

Adenosine receptor A2a (CHEMBL251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

8-(2-Furyl)adenine derivatives as A₂A adenosine receptor ligands.
Dal Ben D, Buccioni M, Lambertucci C, Thomas A, Klotz KN, Federico S, Cacciari B, Spalluto G, Volpini R.
Eur J Med Chem (2013) 70 : 525 -535
PubMed 24189496 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.19 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3087715 1 8.43
CHEMBL3087716 1 8.12
CHEMBL3087707 1 7.82
CHEMBL3087706 1 7.75
CHEMBL3087717 1 7.48
CHEMBL3087711 1 7.30
CHEMBL468633 1 7.28
CHEMBL3087713 1 7.24
CHEMBL3087710 1 7.23
CHEMBL475455 1 7.07
CHEMBL3087712 1 7.05
CHEMBL3087714 1 6.97
CHEMBL3087708 1 6.96
CHEMBL510288 1 6.92
CHEMBL506450 1 6.52
CHEMBL474058 1 6.21
CHEMBL3087709 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3087715 Ki = 3.7 nM 8.43
CHEMBL3087716 Ki = 7.5 nM 8.12
CHEMBL3087707 Ki = 15.0 nM 7.82
CHEMBL3087706 Ki = 18.0 nM 7.75
CHEMBL3087717 Ki = 33.0 nM 7.48
CHEMBL3087711 Ki = 50.0 nM 7.30
CHEMBL468633 Ki = 52.0 nM 7.28
CHEMBL3087713 Ki = 57.0 nM 7.24
CHEMBL3087710 Ki = 59.0 nM 7.23
CHEMBL475455 Ki = 85.0 nM 7.07
CHEMBL3087712 Ki = 89.0 nM 7.05
CHEMBL3087714 Ki = 106.0 nM 6.97
CHEMBL3087708 Ki = 110.0 nM 6.96
CHEMBL510288 Ki = 120.0 nM 6.92
CHEMBL506450 Ki = 300.0 nM 6.52
CHEMBL474058 Ki = 620.0 nM 6.21
CHEMBL3087709 Ki = 1270.0 nM 5.90