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Assay Detail

CHEMBL637241

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Functional
Antagonist activity against adenosine A1 receptor in human platelets
33
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A1 (CHEMBL226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships of 8-cycloalkyl-1,3-dipropylxanthines as antagonists of adenosine receptors.
Katsushima T, Nieves L, Wells JN.
J Med Chem (1990) 33 : 1906 -1910
PubMed 1694546 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 7.45 9.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 9.33
CHEMBL160369 1 8.60
CHEMBL300334 1 8.59
CHEMBL134837 1 8.10
CHEMBL53453 1 8.10
CHEMBL57554 1 7.96
CHEMBL56251 2 7.92
CHEMBL59529 1 7.85
CHEMBL294869 2 7.77
CHEMBL56409 1 7.70
CHEMBL55883 1 7.66
CHEMBL300983 1 7.39
CHEMBL53737 1 7.38
CHEMBL56673 1 7.30
CHEMBL57076 2 7.28
CHEMBL57503 2 7.23
CHEMBL157833 1 7.16
CHEMBL417770 1 7.12
CHEMBL418101 1 7.09
CHEMBL292661 1 7.07
CHEMBL58879 2 7.05
CHEMBL292382 2 7.00
CHEMBL299699 1 6.89
CHEMBL58380 1 6.18
CHEMBL54836 2 -
CHEMBL301403 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 0.47 nM 9.33
CHEMBL160369 Ki = 2.5 nM 8.60
CHEMBL300334 Ki = 2.6 nM 8.59
CHEMBL134837 Ki = 8.0 nM 8.10
CHEMBL53453 Ki = 8.0 nM 8.10
CHEMBL57554 Ki = 11.0 nM 7.96
CHEMBL56251 Ki = 12.0 nM 7.92
CHEMBL59529 Ki = 14.0 nM 7.85
CHEMBL294869 Ki = 17.0 nM 7.77
CHEMBL56409 Ki = 20.0 nM 7.70
CHEMBL55883 Ki = 22.0 nM 7.66
CHEMBL300983 Ki = 41.0 nM 7.39
CHEMBL53737 Ki = 42.0 nM 7.38
CHEMBL56673 Ki = 50.0 nM 7.30
CHEMBL57076 Ki = 53.0 nM 7.28
CHEMBL57503 Ki = 59.0 nM 7.23
CHEMBL56251 Ki = 70.0 nM 7.16
CHEMBL157833 Ki = 69.0 nM 7.16
CHEMBL417770 Ki = 76.0 nM 7.12
CHEMBL418101 Ki = 82.0 nM 7.09
CHEMBL294869 Ki = 85.0 nM 7.07
CHEMBL292661 Ki = 85.0 nM 7.07
CHEMBL58879 Ki = 90.0 nM 7.05
CHEMBL292382 Ki = 100.0 nM 7.00
CHEMBL299699 Ki = 130.0 nM 6.89
CHEMBL292382 Ki = 140.0 nM 6.85
CHEMBL58879 Ki = 160.0 nM 6.80
CHEMBL57503 Ki = 430.0 nM 6.37
CHEMBL58380 Ki = 660.0 nM 6.18
CHEMBL54836 Ki > 3000.0 nM -
CHEMBL57076 Ki > 3000.0 nM -
CHEMBL54836 Ki > 10000.0 nM -
CHEMBL301403 Ki > 10000.0 nM -