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Assay Detail

CHEMBL903347

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
23
Total Activities
23
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

Further studies on the binding of N1-substituted tryptamines at h5-HT6 receptors.
Nyandege A, Kolanos R, Roth BL, Glennon RA.
Bioorg Med Chem Lett (2007) 17 : 1691 -1694
PubMed 17239595 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 7.25 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL94093 1 9.10
CHEMBL393886 1 8.82
CHEMBL247673 1 8.72
CHEMBL248071 1 8.60
CHEMBL93868 1 8.39
CHEMBL188144 1 8.22
CHEMBL247477 1 7.89
CHEMBL248085 1 7.70
CHEMBL395465 1 7.54
CHEMBL365471 1 7.54
CHEMBL247885 1 7.36
CHEMBL396329 1 7.03
CHEMBL247071 1 6.88
CHEMBL397380 1 6.87
CHEMBL435534 1 6.87
CHEMBL247872 1 6.68
CHEMBL248268 1 6.66
CHEMBL245806 1 6.55
CHEMBL247871 1 6.36
CHEMBL247886 1 6.35
CHEMBL394097 1 6.23
CHEMBL396149 1 5.22
CHEMBL247281 1 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL94093 Ki = 0.8 nM 9.10
CHEMBL393886 Ki = 1.5 nM 8.82
CHEMBL247673 Ki = 1.9 nM 8.72
CHEMBL248071 Ki = 2.5 nM 8.60
CHEMBL93868 Ki = 4.1 nM 8.39
CHEMBL188144 Ki = 6.0 nM 8.22
CHEMBL247477 Ki = 13.0 nM 7.89
CHEMBL248085 Ki = 20.0 nM 7.70
CHEMBL395465 Ki = 29.0 nM 7.54
CHEMBL365471 Ki = 29.0 nM 7.54
CHEMBL247885 Ki = 44.0 nM 7.36
CHEMBL396329 Ki = 94.0 nM 7.03
CHEMBL247071 Ki = 132.0 nM 6.88
CHEMBL397380 Ki = 135.0 nM 6.87
CHEMBL435534 Ki = 136.0 nM 6.87
CHEMBL247872 Ki = 210.0 nM 6.68
CHEMBL248268 Ki = 220.0 nM 6.66
CHEMBL245806 Ki = 280.0 nM 6.55
CHEMBL247871 Ki = 440.0 nM 6.36
CHEMBL247886 Ki = 445.0 nM 6.35
CHEMBL394097 Ki = 590.0 nM 6.23
CHEMBL396149 Ki = 6000.0 nM 5.22
CHEMBL247281 Ki = 8200.0 nM 5.09