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Assay Detail

CHEMBL5100443

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

Binding
Inhibition of human TPSO receptor expressed in human HEK293T cell membrane incubated for 90 mins by radioligand binding assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Subcellular Cell membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Translocator protein (CHEMBL5742)
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 2 6.64 6.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5170790 1 6.91
CHEMBL5195535 1 6.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5170790 Ki = 123.0 nM 6.91
CHEMBL5195535 Ki = 427.0 nM 6.37