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Assay Detail

CHEMBL3413556

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

Binding
Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK-293 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 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.
Kołaczkowski M, Marcinkowska M, Bucki A, Śniecikowska J, Pawłowski M, Kazek G, Siwek A, Jastrzębska-Więsek M, Partyka A, Wasik A, Wesołowska A, Mierzejewski P, Bienkowski P.
Eur J Med Chem (2015) 92 : 221 -235
PubMed 25557493 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.79 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56 8-OH-DPAT 1 9.40
CHEMBL3409256 1 8.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56 8-OH-DPAT Ki = 0.4 nM 9.40
CHEMBL3409256 Ki = 6.7 nM 8.17