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Assay Detail

CHEMBL989583

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 by liquid scintillation counting
19
Total Activities
19
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

Indene-based scaffolds. 2. An indole-indene switch: discovery of novel indenylsulfonamides as 5-HT6 serotonin receptor agonists.
Alcalde E, Mesquida N, López-Pérez S, Frigola J, Mercè R.
J Med Chem (2009) 52 : 675 -687
PubMed 19159187 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.93 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175835 1 9.15
CHEMBL392760 1 8.70
CHEMBL76237 1 8.70
CHEMBL362628 1 8.66
CHEMBL457351 1 8.52
CHEMBL93868 1 8.52
CHEMBL476006 1 8.35
CHEMBL188144 1 8.22
CHEMBL515307 1 8.00
CHEMBL431298 1 7.89
CHEMBL267615 1 7.80
CHEMBL478894 1 7.77
CHEMBL478686 1 7.70
CHEMBL478895 1 7.51
CHEMBL433461 1 7.33
CHEMBL457570 1 7.29
CHEMBL477650 1 7.28
CHEMBL457569 1 6.67
CHEMBL478896 1 6.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175835 Ki = 0.7 nM 9.15
CHEMBL392760 Ki = 2.0 nM 8.70
CHEMBL76237 Ki = 2.0 nM 8.70
CHEMBL362628 Ki = 2.2 nM 8.66
CHEMBL457351 Ki = 3.0 nM 8.52
CHEMBL93868 Ki = 3.0 nM 8.52
CHEMBL476006 Ki = 4.5 nM 8.35
CHEMBL188144 Ki = 6.0 nM 8.22
CHEMBL515307 Ki = 10.0 nM 8.00
CHEMBL431298 Ki = 13.0 nM 7.89
CHEMBL267615 Ki = 16.0 nM 7.80
CHEMBL478894 Ki = 17.0 nM 7.77
CHEMBL478686 Ki = 20.0 nM 7.70
CHEMBL478895 Ki = 31.0 nM 7.51
CHEMBL433461 Ki = 47.0 nM 7.33
CHEMBL457570 Ki = 51.0 nM 7.29
CHEMBL477650 Ki = 53.0 nM 7.28
CHEMBL457569 Ki = 216.0 nM 6.67
CHEMBL478896 Ki = 276.0 nM 6.56