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Assay Detail

CHEMBL830246

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

Binding
Displacement of [125I]-AB MECA from recombinant human adenosine A3 receptor expressed in HEK cells
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

2-Pyrazolyl-N(6)-substituted adenosine derivatives as high affinity and selective adenosine A(3) receptor agonists.
Elzein E, Palle V, Wu Y, Maa T, Zeng D, Zablocki J.
J Med Chem (2004) 47 : 4766 -4773
PubMed 15341491 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 7.71 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL119709 IB-MECA 1 8.96
CHEMBL431733 NAMODENOSON 3.0 1 8.85
CHEMBL361072 1 8.70
CHEMBL186443 1 8.70
CHEMBL398587 1 8.70
CHEMBL183940 1 8.52
CHEMBL574597 1 8.47
CHEMBL361938 1 8.22
CHEMBL365642 1 8.00
CHEMBL231677 1 7.82
CHEMBL375190 1 7.80
CHEMBL189069 1 7.72
CHEMBL400414 1 7.39
CHEMBL188454 1 7.31
CHEMBL188482 1 7.22
CHEMBL234790 1 7.14
CHEMBL359991 1 7.01
CHEMBL231891 1 6.97
CHEMBL363458 1 6.96
CHEMBL187300 1 6.83
CHEMBL184557 1 6.80
CHEMBL362117 1 6.77
CHEMBL361075 1 6.50
CHEMBL98278 1 -
CHEMBL318928 1 -
CHEMBL317052 REGADENOSON ANHYDROUS 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL119709 IB-MECA Ki = 1.1 nM 8.96
CHEMBL431733 NAMODENOSON Ki = 1.4 nM 8.85
CHEMBL361072 Ki = 2.0 nM 8.70
CHEMBL186443 Ki = 2.0 nM 8.70
CHEMBL398587 Ki = 2.0 nM 8.70
CHEMBL183940 Ki = 3.0 nM 8.52
CHEMBL574597 Ki = 3.4 nM 8.47
CHEMBL361938 Ki = 6.0 nM 8.22
CHEMBL365642 Ki = 10.0 nM 8.00
CHEMBL231677 Ki = 15.0 nM 7.82
CHEMBL375190 Ki = 16.0 nM 7.80
CHEMBL189069 Ki = 19.0 nM 7.72
CHEMBL400414 Ki = 41.0 nM 7.39
CHEMBL188454 Ki = 49.0 nM 7.31
CHEMBL188482 Ki = 60.0 nM 7.22
CHEMBL234790 Ki = 73.0 nM 7.14
CHEMBL359991 Ki = 97.0 nM 7.01
CHEMBL231891 Ki = 107.0 nM 6.97
CHEMBL363458 Ki = 109.0 nM 6.96
CHEMBL187300 Ki = 148.0 nM 6.83
CHEMBL184557 Ki = 157.0 nM 6.80
CHEMBL362117 Ki = 170.0 nM 6.77
CHEMBL361075 Ki = 320.0 nM 6.50
CHEMBL98278 Ki > 10.0 nM -
CHEMBL318928 Ki > 6.0 nM -
CHEMBL317052 REGADENOSON ANHYDROUS Ki > 10.0 nM -