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Assay Detail

CHEMBL2166697

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

Binding
Binding affinity to human 5-HT6 receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

N,N-Dimethyl-[9-(arylsulfonyl)-2,3,4,9-tetrahydro-1H-carbazol-3-yl]amines as novel, potent and selective 5-HT₆ receptor antagonists.
Nirogi RV, Konda JB, Kambhampati R, Shinde A, Bandyala TR, Gudla P, Kandukuri KK, Jayarajan P, Kandikere V, Dubey PK.
Bioorg Med Chem Lett (2012) 22 : 6980 -6985
PubMed 23036955 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.35 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361213 1 8.85
CHEMBL2165520 1 8.80
CHEMBL92093 1 8.64
CHEMBL76237 1 8.64
CHEMBL127411 1 8.14
CHEMBL2165522 1 7.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361213 Ki = 1.4 nM 8.85
CHEMBL2165520 Ki = 1.6 nM 8.80
CHEMBL92093 Ki = 2.3 nM 8.64
CHEMBL76237 Ki = 2.3 nM 8.64
CHEMBL127411 Ki = 7.2 nM 8.14
CHEMBL2165522 Ki = 96.0 nM 7.02