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Assay Detail

CHEMBL1015328

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A1 (CHEMBL226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N6-Cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine receptor with antinociceptive effects in mice.
Franchetti P, Cappellacci L, Vita P, Petrelli R, Lavecchia A, Kachler S, Klotz KN, Marabese I, Luongo L, Maione S, Grifantini M.
J Med Chem (2009) 52 : 2393 -2406
PubMed 19317449 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.68 9.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL449575 1 9.29
CHEMBL489640 1 9.27
CHEMBL477444 1 9.23
CHEMBL490250 1 9.15
CHEMBL477445 1 8.81
CHEMBL514541 1 8.79
CHEMBL522095 1 8.39
CHEMBL489639 1 8.16
CHEMBL514701 1 8.04
CHEMBL477665 1 8.04
CHEMBL478071 1 7.89
CHEMBL515330 1 7.55
CHEMBL477666 1 7.19
CHEMBL489638 1 6.60
CHEMBL477667 1 6.59
CHEMBL489428 1 5.97
CHEMBL523934 1 5.78
CHEMBL489226 1 5.67
CHEMBL489628 1 5.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL449575 Ki = 0.51 nM 9.29
CHEMBL489640 Ki = 0.54 nM 9.27
CHEMBL477444 Ki = 0.59 nM 9.23
CHEMBL490250 Ki = 0.71 nM 9.15
CHEMBL477445 Ki = 1.56 nM 8.81
CHEMBL514541 Ki = 1.61 nM 8.79
CHEMBL522095 Ki = 4.09 nM 8.39
CHEMBL489639 Ki = 6.96 nM 8.16
CHEMBL514701 Ki = 9.16 nM 8.04
CHEMBL477665 Ki = 9.13 nM 8.04
CHEMBL478071 Ki = 12.8 nM 7.89
CHEMBL515330 Ki = 28.4 nM 7.55
CHEMBL477666 Ki = 64.7 nM 7.19
CHEMBL489638 Ki = 250.0 nM 6.60
CHEMBL477667 Ki = 258.0 nM 6.59
CHEMBL489428 Ki = 1060.0 nM 5.97
CHEMBL523934 Ki = 1680.0 nM 5.78
CHEMBL489226 Ki = 2150.0 nM 5.67
CHEMBL489628 Ki = 2970.0 nM 5.53