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Assay Detail

CHEMBL4308348

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

ADMET
Displacement of [3H]LSD from full length human cloned 5HT6R expressed in HEK293 cells incubated for 1 hr by radioligand displacement assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 6 (CHEMBL3371)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of novel serotonin and dopamine receptor ligands being 6-bromohexyl saccharine derivatives.
Kułaga D, Jaśkowska J, Satała G.
Bioorg Med Chem Lett (2019) 29 : 126667 -126667
PubMed 31547945 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.37 7.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4463030 1 7.28
CHEMBL4440695 1 7.24
CHEMBL4470487 1 6.98
CHEMBL4465181 1 6.88
CHEMBL4454105 1 6.80
CHEMBL4464512 1 6.43
CHEMBL4457109 1 6.34
CHEMBL4569757 1 6.04
CHEMBL4456046 1 6.04
CHEMBL4540404 1 6.01
CHEMBL4462839 1 5.90
CHEMBL4473026 1 5.79
CHEMBL4434735 1 5.76
CHEMBL4592941 1 5.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4463030 Ki = 52.0 nM 7.28
CHEMBL4440695 Ki = 58.0 nM 7.24
CHEMBL4470487 Ki = 104.0 nM 6.98
CHEMBL4465181 Ki = 132.0 nM 6.88
CHEMBL4454105 Ki = 157.0 nM 6.80
CHEMBL4464512 Ki = 372.0 nM 6.43
CHEMBL4457109 Ki = 459.0 nM 6.34
CHEMBL4569757 Ki = 920.0 nM 6.04
CHEMBL4456046 Ki = 921.0 nM 6.04
CHEMBL4540404 Ki = 971.0 nM 6.01
CHEMBL4462839 Ki = 1272.0 nM 5.90
CHEMBL4473026 Ki = 1619.0 nM 5.79
CHEMBL4434735 Ki = 1716.0 nM 5.76
CHEMBL4592941 Ki = 2352.0 nM 5.63