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Assay Detail

CHEMBL1042902

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

Binding
Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortical membrane after 60 mins
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Adenosine receptor A1 (CHEMBL318)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Nucleoside-5'-monophosphates as prodrugs of adenosine A2A receptor agonists activated by ecto-5'-nucleotidase.
El-Tayeb A, Iqbal J, Behrenswerth A, Romio M, Schneider M, Zimmermann H, Schrader J, Müller CE.
J Med Chem (2009) 52 : 7669 -7677
PubMed 19580286 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.30 6.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL567801 1 6.86
CHEMBL577036 1 6.75
CHEMBL577915 1 6.59
CHEMBL568023 1 6.40
CHEMBL576838 1 6.34
CHEMBL568009 1 6.30
CHEMBL578569 1 6.27
CHEMBL578819 1 6.26
CHEMBL577458 1 6.03
CHEMBL576883 1 6.00
CHEMBL578145 1 5.94
CHEMBL577902 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL567801 Ki = 139.0 nM 6.86
CHEMBL577036 Ki = 180.0 nM 6.75
CHEMBL577915 Ki = 256.0 nM 6.59
CHEMBL568023 Ki = 400.0 nM 6.40
CHEMBL576838 Ki = 454.0 nM 6.34
CHEMBL568009 Ki = 498.0 nM 6.30
CHEMBL578569 Ki = 532.0 nM 6.27
CHEMBL578819 Ki = 555.0 nM 6.26
CHEMBL577458 Ki = 927.0 nM 6.03
CHEMBL576883 Ki = 994.0 nM 6.00
CHEMBL578145 Ki = 1140.0 nM 5.94
CHEMBL577902 Ki = 1270.0 nM 5.90