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Assay Detail

CHEMBL640600

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

Binding
Displacement of [3H]CPX from adenosine A1 receptor of calf brain cortical membrane
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A1 (CHEMBL4975)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists.
van Galen PJ, Nissen P, van Wijngaarden I, IJzerman AP, Soudijn W.
J Med Chem (1991) 34 : 1202 -1206
PubMed 2002461 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.18 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19768 1 8.82
CHEMBL62350 8-PHENYL THEOPHYLLINE 1 8.51
CHEMBL19095 1 8.04
CHEMBL19305 1 8.00
CHEMBL276138 1 7.77
CHEMBL442333 1 7.64
CHEMBL441954 1 7.30
CHEMBL1907708 1 7.13
CHEMBL19970 1 6.54
CHEMBL1907924 1 6.34
CHEMBL19533 1 6.31
CHEMBL19191 1 5.77
CHEMBL1355736 THEOPHYLLINE 4.0 1 5.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19768 Ki = 1.5 nM 8.82
CHEMBL62350 8-PHENYL THEOPHYLLINE Ki = 3.1 nM 8.51
CHEMBL19095 Ki = 9.1 nM 8.04
CHEMBL19305 Ki = 10.0 nM 8.00
CHEMBL276138 Ki = 17.0 nM 7.77
CHEMBL442333 Ki = 23.0 nM 7.64
CHEMBL441954 Ki = 50.0 nM 7.30
CHEMBL1907708 Ki = 74.0 nM 7.13
CHEMBL19970 Ki = 290.0 nM 6.54
CHEMBL1907924 Ki = 460.0 nM 6.34
CHEMBL19533 Ki = 490.0 nM 6.31
CHEMBL19191 Ki = 1700.0 nM 5.77
CHEMBL1355736 THEOPHYLLINE Ki = 6000.0 nM 5.22