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Assay Detail

CHEMBL823612

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Functional
Stimulation of [35S]GTP-gamma-S, binding to rat brain membranes by adenosine A1 receptor activation
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A1 (CHEMBL318)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

N-cycloalkyl derivatives of adenosine and 1-deazaadenosine as agonists and partial agonists of the A(1) adenosine receptor.
Vittori S, Lorenzen A, Stannek C, Costanzi S, Volpini R, IJzerman AP, Kunzel JK, Cristalli G.
J Med Chem (2000) 43 : 250 -260
PubMed 10649980 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 6.01 7.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 7.88
CHEMBL284969 1 7.52
CHEMBL2113518 1 7.24
CHEMBL2113430 1 7.06
CHEMBL2113390 1 6.39
CHEMBL608306 1 6.37
CHEMBL2113389 1 6.32
CHEMBL2113521 1 6.15
CHEMBL2113423 1 6.15
CHEMBL2113478 1 5.82
CHEMBL1790734 1 5.81
CHEMBL1790737 1 5.43
CHEMBL1790735 1 5.29
CHEMBL1790733 1 5.24
CHEMBL1790739 1 5.21
CHEMBL611851 1 5.20
CHEMBL312981 1 5.18
CHEMBL1790730 1 5.02
CHEMBL1790715 1 4.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE EC50 = 13.3 nM 7.88
CHEMBL284969 EC50 = 30.0 nM 7.52
CHEMBL2113518 EC50 = 57.3 nM 7.24
CHEMBL2113430 EC50 = 86.4 nM 7.06
CHEMBL2113390 EC50 = 408.0 nM 6.39
CHEMBL608306 EC50 = 431.0 nM 6.37
CHEMBL2113389 EC50 = 475.0 nM 6.32
CHEMBL2113521 EC50 = 704.0 nM 6.15
CHEMBL2113423 EC50 = 709.0 nM 6.15
CHEMBL2113478 EC50 = 1530.0 nM 5.82
CHEMBL1790734 EC50 = 1560.0 nM 5.81
CHEMBL1790737 EC50 = 3710.0 nM 5.43
CHEMBL1790735 EC50 = 5110.0 nM 5.29
CHEMBL1790733 EC50 = 5760.0 nM 5.24
CHEMBL1790739 EC50 = 6180.0 nM 5.21
CHEMBL611851 EC50 = 6360.0 nM 5.20
CHEMBL312981 EC50 = 6580.0 nM 5.18
CHEMBL1790730 EC50 = 9640.0 nM 5.02
CHEMBL1790715 EC50 = 13700.0 nM 4.86