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Assay Detail

CHEMBL3387738

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

Binding
Displacement of [3H]8-OH-DPAT from 5HT1A receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design, synthesis and evaluation of benzo[a]thieno[3,2-g]quinolizines as novel l-SPD derivatives possessing dopamine D1, D2 and serotonin 5-HT1A multiple action profiles.
Li Z, Huang J, Sun H, Zhou S, Guo L, Zhou Y, Zhen X, Liu H.
Bioorg Med Chem (2014) 22 : 5838 -5846
PubMed 25308766 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.36 6.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3344468 1 6.93
CHEMBL3344466 1 6.76
CHEMBL3344469 1 6.54
CHEMBL3344467 1 6.26
CHEMBL3344470 1 6.18
CHEMBL3344465 1 6.11
CHEMBL3344458 1 6.06
CHEMBL3344456 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3344468 Ki = 118.7 nM 6.93
CHEMBL3344466 Ki = 175.32 nM 6.76
CHEMBL3344469 Ki = 285.33 nM 6.54
CHEMBL3344467 Ki = 553.1 nM 6.26
CHEMBL3344470 Ki = 654.64 nM 6.18
CHEMBL3344465 Ki = 777.79 nM 6.11
CHEMBL3344458 Ki = 863.8 nM 6.06
CHEMBL3344456 Ki = 997.7 nM 6.00