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Assay Detail

CHEMBL642860

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

Binding
Binding affinity against rat brain adenosine A1 receptor by using N6-[3H]- cyclohexyladenosine as radioligand
19
Total Activities
19
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

Synthesis of xanthines as adenosine antagonists, a practical quantitative structure-activity relationship application.
Hamilton HW, Ortwine DF, Worth DF, Badger EW, Bristol JA, Bruns RF, Haleen SJ, Steffen RP.
J Med Chem (1985) 28 : 1071 -1079
PubMed 2991519 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.78 8.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL11002 1 8.19
CHEMBL545362 1 8.12
CHEMBL11036 1 8.09
CHEMBL11173 1 7.73
CHEMBL11104 1 7.39
CHEMBL11027 1 7.33
CHEMBL10913 1 7.16
CHEMBL276201 1 6.94
CHEMBL273295 1 6.93
CHEMBL418333 1 6.92
CHEMBL11206 1 6.86
CHEMBL11049 1 6.72
CHEMBL555624 1 6.58
CHEMBL10906 1 6.51
CHEMBL274594 1 6.26
CHEMBL275262 1 6.19
CHEMBL11141 1 5.26
CHEMBL11177 1 5.13
CHEMBL11154 1 4.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL11002 IC50 = 6.5 nM 8.19
CHEMBL545362 IC50 = 7.5 nM 8.12
CHEMBL11036 IC50 = 8.2 nM 8.09
CHEMBL11173 IC50 = 18.5 nM 7.73
CHEMBL11104 IC50 = 41.0 nM 7.39
CHEMBL11027 IC50 = 47.0 nM 7.33
CHEMBL10913 IC50 = 70.0 nM 7.16
CHEMBL276201 IC50 = 116.0 nM 6.94
CHEMBL273295 IC50 = 118.0 nM 6.93
CHEMBL418333 IC50 = 120.0 nM 6.92
CHEMBL11206 IC50 = 138.0 nM 6.86
CHEMBL11049 IC50 = 190.0 nM 6.72
CHEMBL555624 IC50 = 263.0 nM 6.58
CHEMBL10906 IC50 = 310.0 nM 6.51
CHEMBL274594 IC50 = 553.0 nM 6.26
CHEMBL275262 IC50 = 646.0 nM 6.19
CHEMBL11141 IC50 = 5540.0 nM 5.26
CHEMBL11177 IC50 = 7440.0 nM 5.13
CHEMBL11154 IC50 = 30700.0 nM 4.51