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Assay Detail

CHEMBL944975

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
12
Total Activities
12
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 Intermediate

Target

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

Publication

Binding of serotonin and N1-benzenesulfonyltryptamine-related analogs at human 5-HT6 serotonin receptors: receptor modeling studies.
Dukat M, Mosier PD, Kolanos R, Roth BL, Glennon RA.
J Med Chem (2008) 51 : 603 -611
PubMed 18201064 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.92 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL194307 1 9.52
CHEMBL196102 1 8.77
CHEMBL428238 1 8.74
CHEMBL76237 1 8.68
CHEMBL93868 1 8.39
CHEMBL378892 1 7.82
CHEMBL267615 1 7.80
CHEMBL253826 1 7.31
CHEMBL212178 1 7.28
CHEMBL253397 1 7.05
CHEMBL252774 1 7.05
CHEMBL404421 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL194307 Ki = 0.3 nM 9.52
CHEMBL196102 Ki = 1.7 nM 8.77
CHEMBL428238 Ki = 1.8 nM 8.74
CHEMBL76237 Ki = 2.1 nM 8.68
CHEMBL93868 Ki = 4.1 nM 8.39
CHEMBL378892 Ki = 15.0 nM 7.82
CHEMBL267615 Ki = 16.0 nM 7.80
CHEMBL253826 Ki = 49.0 nM 7.31
CHEMBL212178 Ki = 52.0 nM 7.28
CHEMBL253397 Ki = 90.0 nM 7.05
CHEMBL252774 Ki = 90.0 nM 7.05
CHEMBL404421 Ki = 220.0 nM 6.66