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Assay Detail

CHEMBL5100494

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

Binding
Positive allosteric modulator activity in human wild type A3AR receptor stably expressed in human HEK293 cell membrane assessed as inhibition of radioligand [125I]-ABOPX orthosteric binding incubated for 18 hrs in presence of PSB603 by equilibrium radioligand binding assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-Activity Studies of 1<i>H</i>-Imidazo[4,5-<i>c</i>]quinolin-4-amine Derivatives as A<sub>3</sub> Adenosine Receptor Positive Allosteric Modulators.
Fallot LB, Suresh RR, Fisher CL, Salmaso V, O'Connor RD, Kaufman N, Gao ZG, Auchampach JA, Jacobson KA.
J Med Chem (2022) 65 : 15238 -15262
PubMed 36367749 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 5.56 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5177376 1 5.70
CHEMBL475346 1 5.70
CHEMBL5173661 1 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5177376 Ki = 2000.0 nM 5.70
CHEMBL475346 Ki = 2000.0 nM 5.70
CHEMBL5173661 Ki = 5400.0 nM 5.27