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Assay Detail

CHEMBL5099264

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Functional
Agonist activity at human adenosine A2B 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
2
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 A2b (CHEMBL255)
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 5.43 7.28
pEC50 10 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL477 ADENOSINE 4.0 1 7.28
CHEMBL464859 NECA 1 7.20
CHEMBL5195714 1 6.22
CHEMBL5171042 1 6.04
CHEMBL5174429 1 6.01
CHEMBL5203632 1 5.37
CHEMBL5208245 1 5.36
CHEMBL5197358 1 5.31
CHEMBL5205907 1 5.29
CHEMBL5191989 1 5.10
CHEMBL5187330 1 5.10
CHEMBL5186757 1 4.90
CHEMBL5188601 1 4.77
CHEMBL5184828 1 4.72
CHEMBL5174052 1 4.63
CHEMBL5199871 1 4.57
CHEMBL5170857 1 4.42
CHEMBL5206687 1 -
CHEMBL5171285 1 -
CHEMBL5201013 1 -
CHEMBL5172389 1 -
CHEMBL5186981 1 -
CHEMBL5209222 1 -
CHEMBL5182056 1 -
CHEMBL5179726 1 -
CHEMBL5187478 1 -
CHEMBL3771208 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL477 ADENOSINE EC50 = 52.48 nM 7.28
CHEMBL464859 NECA EC50 = 63.1 nM 7.20
CHEMBL5195714 EC50 = 602.56 nM 6.22
CHEMBL5171042 EC50 = 912.01 nM 6.04
CHEMBL5174429 EC50 = 977.24 nM 6.01
CHEMBL5203632 EC50 = 4265.8 nM 5.37
CHEMBL5208245 EC50 = 4365.16 nM 5.36
CHEMBL5197358 EC50 = 4897.79 nM 5.31
CHEMBL5205907 EC50 = 5128.61 nM 5.29
CHEMBL5191989 EC50 = 7943.28 nM 5.10
CHEMBL5187330 EC50 = 7943.28 nM 5.10
CHEMBL5186757 EC50 = 12589.25 nM 4.90
CHEMBL5188601 EC50 = 16982.44 nM 4.77
CHEMBL5184828 EC50 = 19054.61 nM 4.72
CHEMBL5174052 EC50 = 23442.29 nM 4.63
CHEMBL5199871 EC50 = 26915.35 nM 4.57
CHEMBL5170857 EC50 = 38018.94 nM 4.42
CHEMBL5206687 pEC50 - -
CHEMBL5171285 pEC50 - -
CHEMBL5201013 pEC50 - -
CHEMBL5172389 pEC50 - -
CHEMBL5186981 pEC50 - -
CHEMBL5209222 pEC50 - -
CHEMBL5182056 pEC50 - -
CHEMBL5179726 pEC50 - -
CHEMBL5187478 pEC50 - -
CHEMBL3771208 pEC50 - -