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Assay Detail

CHEMBL5099259

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Functional
Agonist activity at human adenosine A1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
31
Total Activities
31
Compounds Tested
1
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 A1 (CHEMBL226)
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 31 8.58 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5174052 1 10.00
CHEMBL5195714 1 9.91
CHEMBL5187330 1 9.88
CHEMBL5172389 1 9.85
CHEMBL5203632 1 9.62
CHEMBL5171042 1 9.53
CHEMBL5174429 1 9.28
CHEMBL5201013 1 9.28
CHEMBL5205907 1 9.21
CHEMBL5197358 1 9.03
CHEMBL5186757 1 8.98
CHEMBL464859 NECA 1 8.96
CHEMBL5187478 1 8.74
CHEMBL5170857 1 8.67
CHEMBL5208245 1 8.67
CHEMBL5199871 1 8.47
CHEMBL3771208 1 8.43
CHEMBL5184828 1 8.29
CHEMBL5184329 1 8.20
CHEMBL5186981 1 8.19
CHEMBL5191989 1 7.99
CHEMBL5206687 1 7.97
CHEMBL5209222 1 7.88
CHEMBL5171835 1 7.87
CHEMBL5188601 1 7.81
CHEMBL5171285 1 7.74
CHEMBL5179726 1 7.74
CHEMBL5183907 1 7.71
CHEMBL5196040 1 7.40
CHEMBL5182056 1 7.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5174052 EC50 = 0.1 nM 10.00
CHEMBL5195714 EC50 = 0.123 nM 9.91
CHEMBL5187330 EC50 = 0.1318 nM 9.88
CHEMBL5172389 EC50 = 0.1413 nM 9.85
CHEMBL5203632 EC50 = 0.2399 nM 9.62
CHEMBL5171042 EC50 = 0.2951 nM 9.53
CHEMBL5174429 EC50 = 0.5248 nM 9.28
CHEMBL5201013 EC50 = 0.5248 nM 9.28
CHEMBL5205907 EC50 = 0.6166 nM 9.21
CHEMBL5197358 EC50 = 0.9333 nM 9.03
CHEMBL5186757 EC50 = 1.047 nM 8.98
CHEMBL464859 NECA EC50 = 1.096 nM 8.96
CHEMBL5187478 EC50 = 1.82 nM 8.74
CHEMBL5170857 EC50 = 2.138 nM 8.67
CHEMBL5208245 EC50 = 2.138 nM 8.67
CHEMBL5199871 EC50 = 3.388 nM 8.47
CHEMBL3771208 EC50 = 3.715 nM 8.43
CHEMBL5184828 EC50 = 5.129 nM 8.29
CHEMBL5184329 EC50 = 6.31 nM 8.20
CHEMBL5186981 EC50 = 6.457 nM 8.19
CHEMBL5191989 EC50 = 10.23 nM 7.99
CHEMBL5206687 EC50 = 10.72 nM 7.97
CHEMBL5209222 EC50 = 13.18 nM 7.88
CHEMBL5171835 EC50 = 13.49 nM 7.87
CHEMBL5188601 EC50 = 15.49 nM 7.81
CHEMBL5171285 EC50 = 18.2 nM 7.74
CHEMBL5179726 EC50 = 18.2 nM 7.74
CHEMBL5183907 EC50 = 19.5 nM 7.71
CHEMBL5196040 EC50 = 39.81 nM 7.40
CHEMBL5182056 EC50 = 40.74 nM 7.39
CHEMBL477 ADENOSINE EC50 = 69.18 nM 7.16