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Assay Detail

CHEMBL618122

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

Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.
Glennon RA, Lee M, Rangisetty JB, Dukat M, Roth BL, Savage JE, McBride A, Rauser L, Hufeisen S, Lee DK.
J Med Chem (2000) 43 : 1011 -1018
PubMed 10715164 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 6.86 7.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL266591 1 7.34
CHEMBL267615 1 7.28
CHEMBL7318 1 7.27
CHEMBL39 SEROTONIN 3.0 1 7.12
CHEMBL7257 MEBUFOTENIN 2.0 1 7.11
CHEMBL7143 1 7.10
CHEMBL8165 5-METHOXYTRYPTAMINE 1 7.06
CHEMBL268800 1 7.01
CHEMBL7173 1 6.89
CHEMBL7228 1 6.78
CHEMBL6640 TRYPTAMINE 1 6.75
CHEMBL7379 1 6.73
CHEMBL7732 1 6.70
CHEMBL7166 1 6.62
CHEMBL7580 1 6.52
CHEMBL7220 1 6.29
CHEMBL7172 1 5.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL266591 Ki = 46.0 nM 7.34
CHEMBL267615 Ki = 52.0 nM 7.28
CHEMBL7318 Ki = 54.0 nM 7.27
CHEMBL39 SEROTONIN Ki = 75.0 nM 7.12
CHEMBL7257 MEBUFOTENIN Ki = 78.0 nM 7.11
CHEMBL7143 Ki = 80.0 nM 7.10
CHEMBL8165 5-METHOXYTRYPTAMINE Ki = 88.0 nM 7.06
CHEMBL268800 Ki = 98.0 nM 7.01
CHEMBL7173 Ki = 130.0 nM 6.89
CHEMBL7228 Ki = 168.0 nM 6.78
CHEMBL6640 TRYPTAMINE Ki = 180.0 nM 6.75
CHEMBL7379 Ki = 185.0 nM 6.73
CHEMBL7732 Ki = 200.0 nM 6.70
CHEMBL7166 Ki = 240.0 nM 6.62
CHEMBL7580 Ki = 300.0 nM 6.52
CHEMBL7220 Ki = 510.0 nM 6.29
CHEMBL7172 Ki = 1030.0 nM 5.99