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Assay Detail

CHEMBL2187071

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

Binding
Displacement of [3H]CCPA from rat adenosine A1 receptor expressed in CHO cells after 60 mins by gamma counter
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications.
Baraldi PG, Preti D, Borea PA, Varani K.
J Med Chem (2012) 55 : 5676 -5703
PubMed 22468757 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.62 8.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2181971 1 8.03
CHEMBL193421 1 8.00
CHEMBL2181970 1 7.80
CHEMBL193692 1 7.36
CHEMBL88147 1 7.28
CHEMBL119709 IB-MECA 1 7.27
CHEMBL1625681 1 6.36
CHEMBL431733 NAMODENOSON 3.0 1 6.09
CHEMBL2181967 1 5.87
CHEMBL138746 1 4.43
CHEMBL108705 1 4.38
CHEMBL265096 1 -
CHEMBL305975 1 -
CHEMBL128929 1 -
CHEMBL89093 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2181971 Ki = 9.4 nM 8.03
CHEMBL193421 Ki = 10.0 nM 8.00
CHEMBL2181970 Ki = 16.0 nM 7.80
CHEMBL193692 Ki = 44.0 nM 7.36
CHEMBL88147 Ki = 53.0 nM 7.28
CHEMBL119709 IB-MECA Ki = 54.0 nM 7.27
CHEMBL1625681 Ki = 440.0 nM 6.36
CHEMBL431733 NAMODENOSON Ki = 820.0 nM 6.09
CHEMBL2181967 Ki = 1350.0 nM 5.87
CHEMBL138746 Ki = 37300.0 nM 4.43
CHEMBL108705 Ki = 41400.0 nM 4.38
CHEMBL265096 Ki > 100000.0 nM -
CHEMBL305975 Ki > 10000.0 nM -
CHEMBL128929 Ki > 10000.0 nM -
CHEMBL89093 Ki > 10000.0 nM -