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Assay Detail

CHEMBL828801

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

Binding
Displacement of [3H]DPCPX binding to adenosine A1 receptors of bovine cortical membranes
21
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A1 (CHEMBL4975)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Synthesis, biological evaluation, and molecular modeling of ribose-modified adenosine analogues as adenosine receptor agonists.
Cappellacci L, Franchetti P, Pasqualini M, Petrelli R, Vita P, Lavecchia A, Novellino E, Costa B, Martini C, Klotz KN, Grifantini M.
J Med Chem (2005) 48 : 1550 -1562
PubMed 15743197 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 6.63 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL251997 1 8.52
CHEMBL400189 1 8.00
CHEMBL119709 IB-MECA 1 7.92
CHEMBL464859 NECA 1 7.85
CHEMBL66393 1 7.64
CHEMBL2113609 1 7.52
CHEMBL444550 2 7.30
CHEMBL2113608 1 6.49
CHEMBL606495 1 6.46
CHEMBL194031 1 6.46
CHEMBL611115 1 6.46
CHEMBL2113641 1 6.34
CHEMBL2113418 1 6.11
CHEMBL431733 NAMODENOSON 3.0 1 6.05
CHEMBL73809 1 5.95
CHEMBL2113640 1 5.88
CHEMBL2113642 1 5.37
CHEMBL2113607 1 5.34
CHEMBL481858 1 5.27
CHEMBL2113643 1 5.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL251997 Ki = 3.0 nM 8.52
CHEMBL400189 Ki = 10.0 nM 8.00
CHEMBL119709 IB-MECA Ki = 12.0 nM 7.92
CHEMBL464859 NECA Ki = 14.0 nM 7.85
CHEMBL66393 Ki = 23.0 nM 7.64
CHEMBL2113609 Ki = 30.0 nM 7.52
CHEMBL444550 Ki = 50.0 nM 7.30
CHEMBL444550 Ki = 85.0 nM 7.07
CHEMBL2113608 Ki = 325.0 nM 6.49
CHEMBL194031 Ki = 350.0 nM 6.46
CHEMBL606495 Ki = 350.0 nM 6.46
CHEMBL611115 Ki = 350.0 nM 6.46
CHEMBL2113641 Ki = 460.0 nM 6.34
CHEMBL2113418 Ki = 770.0 nM 6.11
CHEMBL431733 NAMODENOSON Ki = 890.0 nM 6.05
CHEMBL73809 Ki = 1120.0 nM 5.95
CHEMBL2113640 Ki = 1310.0 nM 5.88
CHEMBL2113642 Ki = 4300.0 nM 5.37
CHEMBL2113607 Ki = 4530.0 nM 5.34
CHEMBL481858 Ki = 5370.0 nM 5.27
CHEMBL2113643 Ki = 5620.0 nM 5.25