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Assay Detail

CHEMBL1028959

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

Binding
Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-activity relationships of truncated D- and l-4'-thioadenosine derivatives as species-independent A3 adenosine receptor antagonists.
Jeong LS, Pal S, Choe SA, Choi WJ, Jacobson KA, Gao ZG, Klutz AM, Hou X, Kim HO, Lee HW, Lee SK, Tosh DK, Moon HR.
J Med Chem (2008) 51 : 6609 -6613
PubMed 18811138 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.34 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL522152 1 9.60
CHEMBL200732 1 9.42
CHEMBL119709 IB-MECA 1 9.00
CHEMBL431733 NAMODENOSON 3.0 1 8.85
CHEMBL494086 1 8.82
CHEMBL500569 1 8.60
CHEMBL493888 1 8.32
CHEMBL226585 1 8.21
CHEMBL387921 1 8.21
CHEMBL522856 1 8.17
CHEMBL509055 1 8.14
CHEMBL436485 1 7.81
CHEMBL226581 1 7.44
CHEMBL388145 1 6.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL522152 Ki = 0.25 nM 9.60
CHEMBL200732 Ki = 0.38 nM 9.42
CHEMBL119709 IB-MECA Ki = 1.0 nM 9.00
CHEMBL431733 NAMODENOSON Ki = 1.4 nM 8.85
CHEMBL494086 Ki = 1.5 nM 8.82
CHEMBL500569 Ki = 2.5 nM 8.60
CHEMBL493888 Ki = 4.8 nM 8.32
CHEMBL226585 Ki = 6.1 nM 8.21
CHEMBL387921 Ki = 6.2 nM 8.21
CHEMBL522856 Ki = 6.8 nM 8.17
CHEMBL509055 Ki = 7.3 nM 8.14
CHEMBL436485 Ki = 15.5 nM 7.81
CHEMBL226581 Ki = 36.2 nM 7.44
CHEMBL388145 Ki = 658.0 nM 6.18