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Assay Detail

CHEMBL4009981

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

Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
8
Total Activities
8
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 6 (CHEMBL3371)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The "Phenylalkylaminome" with a Focus on Selected Drugs of Abuse.
Glennon RA.
J Med Chem (2017) 60 : 2605 -2628
PubMed 28244748 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.87 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2165520 1 8.80
CHEMBL76237 1 8.68
CHEMBL4064950 1 8.60
CHEMBL212063 1 7.68
CHEMBL434365 1 7.42
CHEMBL4063897 1 7.31
CHEMBL209383 1 7.30
CHEMBL415046 1 7.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2165520 Ki = 1.6 nM 8.80
CHEMBL76237 Ki = 2.1 nM 8.68
CHEMBL4064950 Ki = 2.5 nM 8.60
CHEMBL212063 Ki = 21.0 nM 7.68
CHEMBL434365 Ki = 38.0 nM 7.42
CHEMBL4063897 Ki = 49.0 nM 7.31
CHEMBL209383 Ki = 50.0 nM 7.30
CHEMBL415046 Ki = 70.0 nM 7.16