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Assay Detail

CHEMBL828870

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

Binding
Displacement of [125I]AB-MECA from adenosine A3 receptors in bovine cortical membranes
17
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

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 17 6.57 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL431733 NAMODENOSON 3.0 1 9.66
CHEMBL119709 IB-MECA 1 8.06
CHEMBL66393 1 7.82
CHEMBL444550 2 7.19
CHEMBL464859 NECA 1 7.14
CHEMBL400189 1 6.66
CHEMBL194031 1 6.62
CHEMBL2113418 1 6.38
CHEMBL2113608 1 6.32
CHEMBL2113641 1 6.17
CHEMBL2113640 1 5.92
CHEMBL2113609 1 5.59
CHEMBL2113642 1 5.57
CHEMBL2113643 1 5.46
CHEMBL2113607 1 5.24
CHEMBL251997 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL431733 NAMODENOSON Ki = 0.22 nM 9.66
CHEMBL119709 IB-MECA Ki = 8.8 nM 8.06
CHEMBL66393 Ki = 15.2 nM 7.82
CHEMBL444550 Ki = 65.0 nM 7.19
CHEMBL464859 NECA Ki = 73.0 nM 7.14
CHEMBL444550 Ki = 163.0 nM 6.79
CHEMBL400189 Ki = 220.0 nM 6.66
CHEMBL194031 Ki = 240.0 nM 6.62
CHEMBL2113418 Ki = 420.0 nM 6.38
CHEMBL2113608 Ki = 480.0 nM 6.32
CHEMBL2113641 Ki = 670.0 nM 6.17
CHEMBL2113640 Ki = 1200.0 nM 5.92
CHEMBL2113609 Ki = 2560.0 nM 5.59
CHEMBL2113642 Ki = 2700.0 nM 5.57
CHEMBL2113643 Ki = 3510.0 nM 5.46
CHEMBL2113607 Ki = 5780.0 nM 5.24
CHEMBL251997 Ki = 8570.0 nM 5.07