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Assay Detail

CHEMBL3762073

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

Binding
Displacement of [3H]-Raclopride from human D2L receptor expressed in HEK293 cells after 1 hr
5
Total Activities
5
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 Autocuration

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Towards new 5-HT7 antagonists among arylsulfonamide derivatives of (aryloxy)ethyl-alkyl amines: Multiobjective based design, synthesis, and antidepressant and anxiolytic properties.
Canale V, Kurczab R, Partyka A, Satała G, Lenda T, Jastrzębska-Więsek M, Wesołowska A, Bojarski AJ, Zajdel P.
Eur J Med Chem (2016) 108 : 334 -346
PubMed 26698537 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.89 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3759205 1 7.22
CHEMBL3759819 1 7.03
CHEMBL3740054 1 6.99
CHEMBL3759617 1 6.70
CHEMBL3758591 1 6.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3759205 Ki = 60.0 nM 7.22
CHEMBL3759819 Ki = 94.0 nM 7.03
CHEMBL3740054 Ki = 102.0 nM 6.99
CHEMBL3759617 Ki = 199.0 nM 6.70
CHEMBL3758591 Ki = 322.0 nM 6.49