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Assay Detail

CHEMBL638323

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

Binding
Binding affinity carried out with [3H]5'-(N-ethylcarbamoyl)-adenosine in the presence of 50 nM cyclopentyladenosine in rat striatal membranes against adenosine A2 receptor.
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adenosine A2 receptor (CHEMBL2094117)
Type PROTEIN FAMILY
Organism Rattus norvegicus

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 24 5.83 6.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL313780 1 6.39
CHEMBL84363 1 6.37
CHEMBL318537 1 6.36
CHEMBL337073 1 6.32
CHEMBL143710 1 6.24
CHEMBL143622 1 6.24
CHEMBL356458 1 6.23
CHEMBL320668 1 6.16
CHEMBL143567 1 6.00
CHEMBL339270 1 5.96
CHEMBL347787 1 5.92
CHEMBL344992 1 5.85
CHEMBL142410 1 5.82
CHEMBL143565 1 5.75
CHEMBL106937 1 5.57
CHEMBL346382 1 5.48
CHEMBL141486 1 5.40
CHEMBL101800 1 5.20
CHEMBL102371 1 4.85
CHEMBL102372 1 4.54
CHEMBL358971 1 -
CHEMBL345983 1 -
CHEMBL443274 1 -
CHEMBL142576 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL313780 Ki = 410.0 nM 6.39
CHEMBL84363 Ki = 430.0 nM 6.37
CHEMBL318537 Ki = 440.0 nM 6.36
CHEMBL337073 Ki = 480.0 nM 6.32
CHEMBL143710 Ki = 580.0 nM 6.24
CHEMBL143622 Ki = 570.0 nM 6.24
CHEMBL356458 Ki = 590.0 nM 6.23
CHEMBL320668 Ki = 690.0 nM 6.16
CHEMBL143567 Ki = 1000.0 nM 6.00
CHEMBL339270 Ki = 1100.0 nM 5.96
CHEMBL347787 Ki = 1200.0 nM 5.92
CHEMBL344992 Ki = 1400.0 nM 5.85
CHEMBL142410 Ki = 1500.0 nM 5.82
CHEMBL143565 Ki = 1800.0 nM 5.75
CHEMBL106937 Ki = 2700.0 nM 5.57
CHEMBL346382 Ki = 3300.0 nM 5.48
CHEMBL141486 Ki = 4000.0 nM 5.40
CHEMBL101800 Ki = 6300.0 nM 5.20
CHEMBL102371 Ki = 14000.0 nM 4.85
CHEMBL102372 Ki = 29000.0 nM 4.54
CHEMBL358971 Ki > 100000.0 nM -
CHEMBL345983 Ki > 100000.0 nM -
CHEMBL443274 Ki > 100000.0 nM -
CHEMBL142576 Ki > 100000.0 nM -