Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5046638

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

Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Multifunctional Arylsulfone and Arylsulfonamide-Based Ligands with Prominent Mood-Modulating Activity and Benign Safety Profile, Targeting Neuropsychiatric Symptoms of Dementia.
Marcinkowska M, Bucki A, Sniecikowska J, Zagórska A, Fajkis-Zajączkowska N, Siwek A, Gluch-Lutwin M, Żmudzki P, Jastrzebska-Wiesek M, Partyka A, Wesołowska A, Abram M, Przejczowska-Pomierny K, Cios A, Wyska E, Mika K, Kotańska M, Mierzejewski P, Kolaczkowski M.
J Med Chem (2021) 64 : 12603 -12629
PubMed 34436892 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 7.62 9.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93240 METITEPINE 2.0 1 9.03
CHEMBL5077755 1 8.55
CHEMBL5084167 1 8.33
CHEMBL5088232 1 8.11
CHEMBL5092755 1 8.08
CHEMBL5080955 1 8.08
CHEMBL5082267 1 7.87
CHEMBL5089348 1 7.81
CHEMBL5090557 1 7.79
CHEMBL5082182 1 7.78
CHEMBL5080305 1 7.71
CHEMBL5087742 1 7.58
CHEMBL5093017 1 7.36
CHEMBL5077178 1 7.35
CHEMBL5093250 1 7.35
CHEMBL5076882 1 7.26
CHEMBL5076846 1 7.05
CHEMBL5079536 1 7.01
CHEMBL5073337 1 6.99
CHEMBL5080719 1 6.93
CHEMBL5083505 1 6.82
CHEMBL5085390 1 6.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93240 METITEPINE Ki = 0.9333 nM 9.03
CHEMBL5077755 Ki = 2.818 nM 8.55
CHEMBL5084167 Ki = 4.677 nM 8.33
CHEMBL5088232 Ki = 7.762 nM 8.11
CHEMBL5092755 Ki = 8.318 nM 8.08
CHEMBL5080955 Ki = 8.318 nM 8.08
CHEMBL5082267 Ki = 13.49 nM 7.87
CHEMBL5089348 Ki = 15.49 nM 7.81
CHEMBL5090557 Ki = 16.22 nM 7.79
CHEMBL5082182 Ki = 16.6 nM 7.78
CHEMBL5080305 Ki = 19.5 nM 7.71
CHEMBL5087742 Ki = 26.3 nM 7.58
CHEMBL5093017 Ki = 43.65 nM 7.36
CHEMBL5077178 Ki = 44.67 nM 7.35
CHEMBL5093250 Ki = 44.67 nM 7.35
CHEMBL5076882 Ki = 54.95 nM 7.26
CHEMBL5076846 Ki = 89.13 nM 7.05
CHEMBL5079536 Ki = 97.72 nM 7.01
CHEMBL5073337 Ki = 102.33 nM 6.99
CHEMBL5080719 Ki = 117.49 nM 6.93
CHEMBL5083505 Ki = 151.36 nM 6.82
CHEMBL5085390 Ki = 154.88 nM 6.81