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Assay Detail

CHEMBL5100439

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

Binding
Displacement of [3H]-N-methylspiperone from human D3 receptor expressed in human HEK293T cell membrane incubated for 90 mins by 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 HEK293T
Subcellular Cell membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(3) dopamine receptor (CHEMBL234)
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 5.49 6.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5195535 1 6.07
CHEMBL5192606 1 5.28
CHEMBL5170354 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5195535 Ki = 846.0 nM 6.07
CHEMBL5192606 Ki = 5280.0 nM 5.28
CHEMBL5170354 Ki = 7630.0 nM 5.12