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Assay Detail

CHEMBL642431

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Binding
Displacement of specific [3H]CHA binding at adenosine A1 receptor in bovine brain membranes
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Brain membranes
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Synthesis and structure-activity relationships of a new set of 2-arylpyrazolo[3,4-c]quinoline derivatives as adenosine receptor antagonists.
Colotta V, Catarzi D, Varano F, Cecchi L, Filacchioni G, Martini C, Trincavelli L, Lucacchini A.
J Med Chem (2000) 43 : 3118 -3124
PubMed 10956220 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 6.72 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL106520 1 8.49
CHEMBL104115 1 8.07
CHEMBL317270 1 8.03
CHEMBL442005 1 7.65
CHEMBL104425 1 7.57
CHEMBL107414 1 7.39
CHEMBL104177 1 7.26
CHEMBL106986 1 7.22
CHEMBL320805 1 7.16
CHEMBL106906 1 7.14
CHEMBL320741 1 7.12
CHEMBL322263 1 7.07
CHEMBL320283 1 6.97
CHEMBL321441 1 6.96
CHEMBL107446 1 6.89
CHEMBL107116 1 6.88
CHEMBL419002 1 6.83
CHEMBL107571 1 6.73
CHEMBL106346 1 6.67
CHEMBL105913 1 6.62
CHEMBL104478 1 6.55
CHEMBL106740 1 6.33
CHEMBL318323 1 6.32
CHEMBL107637 1 6.28
CHEMBL322228 1 6.23
CHEMBL387592 1 6.08
CHEMBL320093 1 6.02
CHEMBL242203 1 5.97
CHEMBL106040 1 5.91
CHEMBL108178 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL106520 Ki = 3.2 nM 8.49
CHEMBL104115 Ki = 8.6 nM 8.07
CHEMBL317270 Ki = 9.3 nM 8.03
CHEMBL442005 Ki = 22.2 nM 7.65
CHEMBL104425 Ki = 27.1 nM 7.57
CHEMBL107414 Ki = 40.7 nM 7.39
CHEMBL104177 Ki = 54.7 nM 7.26
CHEMBL106986 Ki = 60.1 nM 7.22
CHEMBL320805 Ki = 69.2 nM 7.16
CHEMBL106906 Ki = 71.9 nM 7.14
CHEMBL320741 Ki = 75.9 nM 7.12
CHEMBL322263 Ki = 86.1 nM 7.07
CHEMBL320283 Ki = 107.0 nM 6.97
CHEMBL321441 Ki = 110.0 nM 6.96
CHEMBL107446 Ki = 129.0 nM 6.89
CHEMBL107116 Ki = 132.0 nM 6.88
CHEMBL419002 Ki = 148.0 nM 6.83
CHEMBL107571 Ki = 186.0 nM 6.73
CHEMBL106346 Ki = 215.0 nM 6.67
CHEMBL105913 Ki = 238.0 nM 6.62
CHEMBL104478 Ki = 284.0 nM 6.55
CHEMBL106740 Ki = 464.0 nM 6.33
CHEMBL318323 Ki = 478.0 nM 6.32
CHEMBL107637 Ki = 520.0 nM 6.28
CHEMBL322228 Ki = 583.0 nM 6.23
CHEMBL387592 Ki = 830.0 nM 6.08
CHEMBL320093 Ki = 950.0 nM 6.02
CHEMBL242203 Ki = 1078.0 nM 5.97
CHEMBL106040 Ki = 1230.0 nM 5.91
CHEMBL108178 Ki = 1500.0 nM 5.82
CHEMBL241987 Ki = 2100.0 nM 5.68
CHEMBL104178 Ki = 2290.0 nM 5.64
CHEMBL324419 Ki = 3200.0 nM 5.50
CHEMBL242202 Ki = 3900.0 nM 5.41