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Assay Detail

CHEMBL829048

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

Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
14
Total Activities
14
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 Expert

Target

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

Publication

Binding of isotryptamines and indenes at h5-HT6 serotonin receptors.
Kolanos R, Siripurapu U, Pullagurla M, Riaz M, Setola V, Roth BL, Dukat M, Glennon RA.
Bioorg Med Chem Lett (2005) 15 : 1987 -1991
PubMed 15808453 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.61 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL194174 1 8.52
CHEMBL188144 1 8.22
CHEMBL371978 1 7.92
CHEMBL186621 1 7.50
CHEMBL193841 1 7.30
CHEMBL427354 1 7.24
CHEMBL195317 1 7.00
CHEMBL193376 1 6.19
CHEMBL191972 1 6.13
CHEMBL364248 1 5.60
CHEMBL191844 1 5.38
CHEMBL193637 1 5.35
CHEMBL364089 1 5.21
CHEMBL371048 1 4.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL194174 Ki = 3.0 nM 8.52
CHEMBL188144 Ki = 6.0 nM 8.22
CHEMBL371978 Ki = 12.0 nM 7.92
CHEMBL186621 Ki = 32.0 nM 7.50
CHEMBL193841 Ki = 50.0 nM 7.30
CHEMBL427354 Ki = 57.0 nM 7.24
CHEMBL195317 Ki = 100.0 nM 7.00
CHEMBL193376 Ki = 640.0 nM 6.19
CHEMBL191972 Ki = 740.0 nM 6.13
CHEMBL364248 Ki = 2530.0 nM 5.60
CHEMBL191844 Ki = 4200.0 nM 5.38
CHEMBL193637 Ki = 4470.0 nM 5.35
CHEMBL364089 Ki = 6100.0 nM 5.21
CHEMBL371048 Ki = 11800.0 nM 4.93