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Assay Detail

CHEMBL641989

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

Binding
Binding affinity against adenosine A2 receptor of striatal membrane using [3H]CGS-21680 as a radioligand
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adenosine A2 receptor (CHEMBL2094257)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position.
Miyamoto K, Yamamoto Y, Kurita M, Sakai R, Konno K, Sanae F, Ohshima T, Takagi K, Hasegawa T, Iwasaki N.
J Med Chem (1993) 36 : 1380 -1386
PubMed 8496906 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 40 4.79 5.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157655 1 5.62
CHEMBL29518 1 5.50
CHEMBL28194 1 5.41
CHEMBL28980 1 5.25
CHEMBL286976 1 5.10
CHEMBL29461 1 4.93
CHEMBL287180 1 4.92
CHEMBL28075 1 4.92
CHEMBL28879 1 4.89
CHEMBL445847 1 4.80
CHEMBL1355736 THEOPHYLLINE 4.0 1 4.78
CHEMBL283412 1 4.67
CHEMBL29272 1 4.67
CHEMBL283024 1 4.64
CHEMBL282310 1 4.36
CHEMBL28298 1 4.23
CHEMBL283454 1 4.16
CHEMBL288786 1 4.09
CHEMBL279898 ENPROFYLLINE 2.0 1 4.04
CHEMBL283020 1 -
CHEMBL281972 1 -
CHEMBL28683 1 -
CHEMBL32184 1 -
CHEMBL286741 1 -
CHEMBL31838 1 -
CHEMBL29052 1 -
CHEMBL31859 1 -
CHEMBL29209 1 -
CHEMBL27967 1 -
CHEMBL28419 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157655 Ki = 2400.0 nM 5.62
CHEMBL29518 Ki = 3200.0 nM 5.50
CHEMBL28194 Ki = 3900.0 nM 5.41
CHEMBL28980 Ki = 5600.0 nM 5.25
CHEMBL286976 Ki = 8000.0 nM 5.10
CHEMBL29461 Ki = 11800.0 nM 4.93
CHEMBL287180 Ki = 12100.0 nM 4.92
CHEMBL28075 Ki = 12000.0 nM 4.92
CHEMBL28879 Ki = 12800.0 nM 4.89
CHEMBL445847 Ki = 15700.0 nM 4.80
CHEMBL1355736 THEOPHYLLINE Ki = 16600.0 nM 4.78
CHEMBL283412 Ki = 21500.0 nM 4.67
CHEMBL29272 Ki = 21600.0 nM 4.67
CHEMBL283024 Ki = 22900.0 nM 4.64
CHEMBL282310 Ki = 43800.0 nM 4.36
CHEMBL28298 Ki = 58700.0 nM 4.23
CHEMBL283454 Ki = 68700.0 nM 4.16
CHEMBL288786 Ki = 81500.0 nM 4.09
CHEMBL279898 ENPROFYLLINE Ki = 90600.0 nM 4.04
CHEMBL282160 Ki > 200000.0 nM -
CHEMBL28684 Ki > 200000.0 nM -
CHEMBL27970 Ki > 200000.0 nM -
CHEMBL28295 Ki > 200000.0 nM -
CHEMBL28300 Ki > 200000.0 nM -
CHEMBL28603 Ki > 200000.0 nM -
CHEMBL32241 Ki = 162000.0 nM -
CHEMBL27915 Ki > 200000.0 nM -
CHEMBL27969 Ki > 200000.0 nM -
CHEMBL282394 Ki = 144000.0 nM -
CHEMBL28419 Ki > 200000.0 nM -
CHEMBL27967 Ki > 200000.0 nM -
CHEMBL29209 Ki > 200000.0 nM -
CHEMBL31859 Ki > 200000.0 nM -
CHEMBL29052 Ki > 200000.0 nM -
CHEMBL31838 Ki > 200000.0 nM -
CHEMBL286741 Ki > 200000.0 nM -
CHEMBL32184 Ki > 200000.0 nM -
CHEMBL28683 Ki > 200000.0 nM -
CHEMBL281972 Ki > 200000.0 nM -
CHEMBL283020 Ki > 200000.0 nM -