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Assay Detail

CHEMBL3297333

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

Binding
Displacement of [3H]8-OH-DPAT from human recombinant 5-HT1A receptor expressed in HEK293 cells
2
Total Activities
2
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

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel arylsulfonamide derivatives with 5-HT₆/5-HT₇ receptor antagonism targeting behavioral and psychological symptoms of dementia.
Kołaczkowski M, Marcinkowska M, Bucki A, Pawłowski M, Mitka K, Jaśkowska J, Kowalski P, Kazek G, Siwek A, Wasik A, Wesołowska A, Mierzejewski P, Bienkowski P.
J Med Chem (2014) 57 : 4543 -4557
PubMed 24805037 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.18 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56 8-OH-DPAT 1 9.40
CHEMBL3290012 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56 8-OH-DPAT Ki = 0.4 nM 9.40
CHEMBL3290012 Ki = 110.0 nM 6.96