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Assay Detail

CHEMBL642335

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

Binding
Inhibition of NECA binding to adenosine A2 receptor mediates reduced adenylate cyclase activity in human platelets
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Adenosine A2 receptor (CHEMBL2094257)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

125I-labeled 8-phenylxanthine derivatives: antagonist radioligands for adenosine A1 receptors.
Linden J, Patel A, Earl CQ, Craig RH, Daluge SM.
J Med Chem (1988) 31 : 745 -751
PubMed 3351850 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 5.36 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL355370 1 6.16
CHEMBL27041 1 6.10
CHEMBL349519 1 6.00
CHEMBL162814 1 5.75
CHEMBL162658 1 5.68
CHEMBL162558 1 5.28
CHEMBL161933 1 5.28
CHEMBL164623 1 5.27
CHEMBL162986 1 4.94
CHEMBL351481 1 4.94
CHEMBL353115 1 4.91
CHEMBL162702 1 4.70
CHEMBL163574 1 4.64
CHEMBL161934 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL355370 Ki = 700.0 nM 6.16
CHEMBL27041 Ki = 800.0 nM 6.10
CHEMBL349519 Ki = 1000.0 nM 6.00
CHEMBL162814 Ki = 1800.0 nM 5.75
CHEMBL162658 Ki = 2100.0 nM 5.68
CHEMBL162558 Ki = 5300.0 nM 5.28
CHEMBL161933 Ki = 5300.0 nM 5.28
CHEMBL164623 Ki = 5400.0 nM 5.27
CHEMBL162986 Ki = 11500.0 nM 4.94
CHEMBL351481 Ki = 11500.0 nM 4.94
CHEMBL353115 Ki = 12300.0 nM 4.91
CHEMBL162702 Ki = 20000.0 nM 4.70
CHEMBL163574 Ki = 23000.0 nM 4.64
CHEMBL161934 Ki > 100000.0 nM -