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Assay Detail

CHEMBL5099262

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Functional
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
27
Total Activities
27
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery and Structure-Activity Relationship Studies of Novel Adenosine A<sub>1</sub> Receptor-Selective Agonists.
Preti B, Suchankova A, Deganutti G, Leuenberger M, Barkan K, Manulak I, Huang X, Carvalho S, Ladds G, Lochner M.
J Med Chem (2022) 65 : 14864 -14890
PubMed 36270633 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 5.60 7.95
pEC50 7 - -
Activity 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL464859 NECA 1 7.95
CHEMBL477 ADENOSINE 4.0 1 7.60
CHEMBL5205907 1 6.26
CHEMBL5197358 1 5.96
CHEMBL5174429 1 5.86
CHEMBL5208245 1 5.68
CHEMBL5195714 1 5.67
CHEMBL5171042 1 5.48
CHEMBL5201013 1 5.24
CHEMBL5187330 1 5.20
CHEMBL5199871 1 5.17
CHEMBL5184828 1 5.04
CHEMBL3771208 1 4.95
CHEMBL5191989 1 4.86
CHEMBL5186981 1 4.86
CHEMBL5188601 1 4.84
CHEMBL5203632 1 4.58
CHEMBL5171285 1 -
CHEMBL5174052 1 -
CHEMBL5186757 1 -
CHEMBL5206687 1 -
CHEMBL5172389 1 -
CHEMBL5170857 1 -
CHEMBL5209222 1 -
CHEMBL5182056 1 -
CHEMBL5179726 1 -
CHEMBL5187478 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL464859 NECA EC50 = 11.22 nM 7.95
CHEMBL477 ADENOSINE EC50 = 25.12 nM 7.60
CHEMBL5205907 EC50 = 549.54 nM 6.26
CHEMBL5197358 EC50 = 1096.48 nM 5.96
CHEMBL5174429 EC50 = 1380.38 nM 5.86
CHEMBL5208245 EC50 = 2089.3 nM 5.68
CHEMBL5195714 EC50 = 2137.96 nM 5.67
CHEMBL5171042 EC50 = 3311.31 nM 5.48
CHEMBL5201013 EC50 = 5754.4 nM 5.24
CHEMBL5187330 EC50 = 6309.57 nM 5.20
CHEMBL5199871 EC50 = 6760.83 nM 5.17
CHEMBL5184828 EC50 = 9120.11 nM 5.04
CHEMBL3771208 EC50 = 11220.18 nM 4.95
CHEMBL5191989 EC50 = 13803.84 nM 4.86
CHEMBL5186981 EC50 = 13803.84 nM 4.86
CHEMBL5188601 EC50 = 14454.4 nM 4.84
CHEMBL5203632 EC50 = 26302.68 nM 4.58
CHEMBL5171285 pEC50 - -
CHEMBL5174052 pEC50 - -
CHEMBL5186757 pEC50 - -
CHEMBL5206687 pEC50 - -
CHEMBL5172389 Activity - -
CHEMBL5170857 Activity - -
CHEMBL5209222 pEC50 - -
CHEMBL5182056 pEC50 - -
CHEMBL5179726 Activity - -
CHEMBL5187478 pEC50 - -