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Assay Detail

CHEMBL637713

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Binding
Binding affinity for adenosine A1 receptor, was assessed from the ability to displace [3H]DPCPX (with 1 mM GTP) from rat cortical membranes.
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 12 5.24 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1790716 1 5.96
CHEMBL1790734 1 5.88
CHEMBL1790714 1 5.85
CHEMBL1790736 1 5.59
CHEMBL1790737 1 5.44
CHEMBL1790731 1 5.03
CHEMBL1790733 1 4.99
CHEMBL1790739 1 4.84
CHEMBL1790730 1 4.78
CHEMBL1790715 1 4.69
CHEMBL1790735 1 4.63
CHEMBL1790738 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1790716 Ki = 1090.0 nM 5.96
CHEMBL1790734 Ki = 1320.0 nM 5.88
CHEMBL1790714 Ki = 1410.0 nM 5.85
CHEMBL1790736 Ki = 2560.0 nM 5.59
CHEMBL1790737 Ki = 3600.0 nM 5.44
CHEMBL1790731 Ki = 9310.0 nM 5.03
CHEMBL1790733 Ki = 10200.0 nM 4.99
CHEMBL1790739 Ki = 14300.0 nM 4.84
CHEMBL1790730 Ki = 16700.0 nM 4.78
CHEMBL1790715 Ki = 20400.0 nM 4.69
CHEMBL1790735 Ki = 23600.0 nM 4.63
CHEMBL1790738 Ki = 134000.0 nM -