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Assay Detail

CHEMBL3413616

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

Binding
Displacement of [125I]I-AB-MECA from human recombinant A3 adenosine receptor expressed in CHO cells after 60 mins by liquid scintillation counting
33
Total Activities
33
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

In vivo phenotypic screening for treating chronic neuropathic pain: modification of C2-arylethynyl group of conformationally constrained A3 adenosine receptor agonists.
Tosh DK, Finley A, Paoletta S, Moss SM, Gao ZG, Gizewski ET, Auchampach JA, Salvemini D, Jacobson KA.
J Med Chem (2014) 57 : 9901 -9914
PubMed 25422861 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 8.89 9.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3407785 1 9.36
CHEMBL3407782 1 9.28
CHEMBL2064639 1 9.28
CHEMBL2064640 1 9.24
CHEMBL3407783 1 9.24
CHEMBL3407778 1 9.21
CHEMBL3407768 1 9.20
CHEMBL3407784 1 9.15
CHEMBL3407766 1 9.11
CHEMBL2064635 1 9.07
CHEMBL3407767 1 9.04
CHEMBL2064637 1 9.01
CHEMBL2064638 1 9.01
CHEMBL2064636 1 9.00
CHEMBL3407787 1 8.94
CHEMBL2064642 1 8.91
CHEMBL3407779 1 8.84
CHEMBL3407780 1 8.82
CHEMBL3407781 1 8.79
CHEMBL3407788 1 8.78
CHEMBL2064645 1 8.78
CHEMBL3407774 1 8.75
CHEMBL3407773 1 8.71
CHEMBL3407772 1 8.68
CHEMBL3407786 1 8.68
CHEMBL3407771 1 8.67
CHEMBL3407770 1 8.67
CHEMBL3407776 1 8.65
CHEMBL3407777 1 8.63
CHEMBL2064650 1 8.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3407785 Ki = 0.44 nM 9.36
CHEMBL3407782 Ki = 0.52 nM 9.28
CHEMBL2064639 Ki = 0.53 nM 9.28
CHEMBL2064640 Ki = 0.58 nM 9.24
CHEMBL3407783 Ki = 0.57 nM 9.24
CHEMBL3407778 Ki = 0.62 nM 9.21
CHEMBL3407768 Ki = 0.63 nM 9.20
CHEMBL3407784 Ki = 0.7 nM 9.15
CHEMBL3407766 Ki = 0.77 nM 9.11
CHEMBL2064635 Ki = 0.85 nM 9.07
CHEMBL3407767 Ki = 0.91 nM 9.04
CHEMBL2064637 Ki = 0.97 nM 9.01
CHEMBL2064638 Ki = 0.97 nM 9.01
CHEMBL2064636 Ki = 1.01 nM 9.00
CHEMBL3407787 Ki = 1.15 nM 8.94
CHEMBL2064642 Ki = 1.22 nM 8.91
CHEMBL3407779 Ki = 1.45 nM 8.84
CHEMBL3407780 Ki = 1.5 nM 8.82
CHEMBL3407781 Ki = 1.62 nM 8.79
CHEMBL3407788 Ki = 1.68 nM 8.78
CHEMBL2064645 Ki = 1.65 nM 8.78
CHEMBL3407774 Ki = 1.76 nM 8.75
CHEMBL3407773 Ki = 1.97 nM 8.71
CHEMBL3407772 Ki = 2.07 nM 8.68
CHEMBL3407786 Ki = 2.1 nM 8.68
CHEMBL3407771 Ki = 2.15 nM 8.67
CHEMBL3407770 Ki = 2.16 nM 8.67
CHEMBL3407776 Ki = 2.23 nM 8.65
CHEMBL3407777 Ki = 2.34 nM 8.63
CHEMBL2064650 Ki = 3.1 nM 8.51
CHEMBL3407769 Ki = 3.39 nM 8.47
CHEMBL2064657 Ki = 3.49 nM 8.46
CHEMBL3407775 Ki = 3.53 nM 8.45