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Assay Detail

CHEMBL2187073

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

Binding
Displacement of [3H]CGS21680 from rat adenosine A2A receptor expressed in CHO cells after 60 mins by gamma counter
13
Total Activities
13
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 A2a (CHEMBL302)
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 13 6.29 7.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2181971 1 7.48
CHEMBL119709 IB-MECA 1 7.25
CHEMBL193692 1 7.12
CHEMBL2181970 1 6.34
CHEMBL431733 NAMODENOSON 3.0 1 6.33
CHEMBL1625681 1 5.68
CHEMBL193421 1 5.53
CHEMBL108705 1 4.62
CHEMBL305975 1 -
CHEMBL128929 1 -
CHEMBL89093 1 -
CHEMBL265096 1 -
CHEMBL138746 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2181971 Ki = 33.0 nM 7.48
CHEMBL119709 IB-MECA Ki = 56.0 nM 7.25
CHEMBL193692 Ki = 75.0 nM 7.12
CHEMBL2181970 Ki = 459.0 nM 6.34
CHEMBL431733 NAMODENOSON Ki = 470.0 nM 6.33
CHEMBL1625681 Ki = 2100.0 nM 5.68
CHEMBL193421 Ki = 2980.0 nM 5.53
CHEMBL108705 Ki = 24100.0 nM 4.62
CHEMBL305975 Ki > 10000.0 nM -
CHEMBL128929 Ki > 10000.0 nM -
CHEMBL89093 Ki > 10000.0 nM -
CHEMBL265096 Ki > 10000.0 nM -
CHEMBL138746 Ki > 10000.0 nM -