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Assay Detail

CHEMBL640356

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

Binding
Binding affinity carried out with [3H]cyclohexyladenosine in guinea pig forebrain membranes against adenosine A1 receptor
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Subcellular Brain membranes
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Adenosine receptor A1 (CHEMBL2304404)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

8-(Dicyclopropylmethyl)-1,3-dipropylxanthine: a potent and selective adenosine A1 antagonist with renal protective and diuretic activities.
Shimada J, Suzuki F, Nonaka H, Karasawa A, Mizumoto H, Ohno T, Kubo K, Ishii A.
J Med Chem (1991) 34 : 466 -469
PubMed 1992150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 6.79 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL84363 1 8.52
CHEMBL318537 1 8.26
CHEMBL143567 1 8.01
CHEMBL313780 1 7.92
CHEMBL320668 1 7.89
CHEMBL143622 1 7.72
CHEMBL347787 1 7.60
CHEMBL142410 1 7.31
CHEMBL356458 1 7.11
CHEMBL106937 1 7.09
CHEMBL339270 1 7.00
CHEMBL143565 1 6.82
CHEMBL143710 1 6.66
CHEMBL342782 1 6.60
CHEMBL344992 1 6.60
CHEMBL337073 1 6.58
CHEMBL141486 1 6.40
CHEMBL346382 1 6.05
CHEMBL443274 1 5.89
CHEMBL102371 1 5.80
CHEMBL423016 1 5.68
CHEMBL345983 1 5.52
CHEMBL102372 1 5.13
CHEMBL101800 1 4.89
CHEMBL142576 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL84363 Ki = 3.0 nM 8.52
CHEMBL318537 Ki = 5.5 nM 8.26
CHEMBL143567 Ki = 9.7 nM 8.01
CHEMBL313780 Ki = 12.0 nM 7.92
CHEMBL320668 Ki = 13.0 nM 7.89
CHEMBL143622 Ki = 19.0 nM 7.72
CHEMBL347787 Ki = 25.0 nM 7.60
CHEMBL142410 Ki = 49.0 nM 7.31
CHEMBL356458 Ki = 78.0 nM 7.11
CHEMBL106937 Ki = 81.0 nM 7.09
CHEMBL339270 Ki = 100.0 nM 7.00
CHEMBL143565 Ki = 150.0 nM 6.82
CHEMBL143710 Ki = 220.0 nM 6.66
CHEMBL342782 Ki = 250.0 nM 6.60
CHEMBL344992 Ki = 250.0 nM 6.60
CHEMBL337073 Ki = 260.0 nM 6.58
CHEMBL141486 Ki = 400.0 nM 6.40
CHEMBL346382 Ki = 900.0 nM 6.05
CHEMBL443274 Ki = 1300.0 nM 5.89
CHEMBL102371 Ki = 1600.0 nM 5.80
CHEMBL423016 Ki = 2100.0 nM 5.68
CHEMBL345983 Ki = 3000.0 nM 5.52
CHEMBL102372 Ki = 7400.0 nM 5.13
CHEMBL101800 Ki = 13000.0 nM 4.89
CHEMBL142576 Ki > 100000.0 nM -