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Assay Detail

CHEMBL640253

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

Binding
Inhibition of specific binding of [3H]CPX to the A1 adenosine receptor in DDT1 MF-2 (DDT) cells.
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cricetulus griseus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Substituted 1,3-dipropylxanthines as irreversible antagonists of A1 adenosine receptors.
Scammells PJ, Baker SP, Belardinelli L, Olsson RA.
J Med Chem (1994) 37 : 2704 -2712
PubMed 8064798 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 6.27 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL328953 1 8.10
CHEMBL329774 1 8.05
CHEMBL327708 1 8.00
CHEMBL91604 1 7.96
CHEMBL88128 1 7.70
CHEMBL90627 1 7.70
CHEMBL94105 1 7.22
CHEMBL314539 1 7.10
CHEMBL90702 1 7.06
CHEMBL90024 1 7.05
CHEMBL92906 1 6.22
CHEMBL329810 1 6.16
CHEMBL330335 1 6.16
CHEMBL89920 1 6.10
CHEMBL91505 1 5.92
CHEMBL91284 1 5.70
CHEMBL446355 1 5.66
CHEMBL90037 1 5.60
CHEMBL90720 1 5.58
CHEMBL93600 1 5.46
CHEMBL328033 1 5.46
CHEMBL93674 1 5.40
CHEMBL90745 1 5.38
CHEMBL90298 1 5.20
CHEMBL90937 1 5.16
CHEMBL91135 1 4.96
CHEMBL89939 1 4.85
CHEMBL94284 1 4.77
CHEMBL94234 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL328953 IC50 = 8.0 nM 8.10
CHEMBL329774 IC50 = 9.0 nM 8.05
CHEMBL327708 IC50 = 10.0 nM 8.00
CHEMBL91604 IC50 = 11.0 nM 7.96
CHEMBL88128 IC50 = 20.0 nM 7.70
CHEMBL90627 IC50 = 20.0 nM 7.70
CHEMBL94105 IC50 = 60.0 nM 7.22
CHEMBL314539 IC50 = 80.0 nM 7.10
CHEMBL90702 IC50 = 87.0 nM 7.06
CHEMBL90024 IC50 = 90.0 nM 7.05
CHEMBL92906 IC50 = 600.0 nM 6.22
CHEMBL329810 IC50 = 700.0 nM 6.16
CHEMBL330335 IC50 = 700.0 nM 6.16
CHEMBL89920 IC50 = 800.0 nM 6.10
CHEMBL91505 IC50 = 1200.0 nM 5.92
CHEMBL91284 IC50 = 2000.0 nM 5.70
CHEMBL446355 IC50 = 2200.0 nM 5.66
CHEMBL90037 IC50 = 2500.0 nM 5.60
CHEMBL90720 IC50 = 2600.0 nM 5.58
CHEMBL93600 IC50 = 3500.0 nM 5.46
CHEMBL328033 IC50 = 3500.0 nM 5.46
CHEMBL93674 IC50 = 4000.0 nM 5.40
CHEMBL90745 IC50 = 4200.0 nM 5.38
CHEMBL90298 IC50 = 6300.0 nM 5.20
CHEMBL90937 IC50 = 7000.0 nM 5.16
CHEMBL91135 IC50 = 11000.0 nM 4.96
CHEMBL89939 IC50 = 14000.0 nM 4.85
CHEMBL94284 IC50 = 17000.0 nM 4.77
CHEMBL94234 IC50 > 100000.0 nM -