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Assay Detail

CHEMBL899100

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 HeLa cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist.
Cole DC, Stock JR, Lennox WJ, Bernotas RC, Ellingboe JW, Boikess S, Coupet J, Smith DL, Leung L, Zhang GM, Feng X, Kelly MF, Galante R, Huang P, Dawson LA, Marquis K, Rosenzweig-Lipson S, Beyer CE, Schechter LE.
J Med Chem (2007) 50 : 5535 -5538
PubMed 17948978 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 8.07 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL236987 1 9.00
CHEMBL392760 1 8.70
CHEMBL76237 1 8.64
CHEMBL93868 1 8.54
CHEMBL236989 1 8.22
CHEMBL235986 1 8.22
CHEMBL236990 1 8.15
CHEMBL236988 1 8.15
CHEMBL394303 1 8.10
CHEMBL238277 1 8.00
CHEMBL238770 1 8.00
CHEMBL363275 1 8.00
CHEMBL366151 1 7.99
CHEMBL235985 1 7.96
CHEMBL235987 1 7.85
CHEMBL392844 1 7.80
CHEMBL394302 1 7.68
CHEMBL395145 1 7.52
CHEMBL446194 1 7.51
CHEMBL236986 1 7.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL236987 Ki = 1.0 nM 9.00
CHEMBL392760 Ki = 2.0 nM 8.70
CHEMBL76237 Ki = 2.3 nM 8.64
CHEMBL93868 Ki = 2.9 nM 8.54
CHEMBL236989 Ki = 6.0 nM 8.22
CHEMBL235986 Ki = 6.0 nM 8.22
CHEMBL236990 Ki = 7.0 nM 8.15
CHEMBL236988 Ki = 7.0 nM 8.15
CHEMBL394303 Ki = 8.0 nM 8.10
CHEMBL238277 Ki = 10.0 nM 8.00
CHEMBL238770 Ki = 10.0 nM 8.00
CHEMBL363275 Ki = 10.0 nM 8.00
CHEMBL366151 Ki = 10.3 nM 7.99
CHEMBL235985 Ki = 11.0 nM 7.96
CHEMBL235987 Ki = 14.0 nM 7.85
CHEMBL392844 Ki = 16.0 nM 7.80
CHEMBL394302 Ki = 21.0 nM 7.68
CHEMBL395145 Ki = 30.0 nM 7.52
CHEMBL446194 Ki = 31.0 nM 7.51
CHEMBL236986 Ki = 47.0 nM 7.33