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Assay Detail

CHEMBL829617

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

Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected 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 Expert

Target

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

Publication

1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-indoles as novel 5-HT6 receptor ligands.
Bernotas R, Lenicek S, Antane S, Zhang GM, Smith D, Coupet J, Harrison B, Schechter LE.
Bioorg Med Chem Lett (2004) 14 : 5499 -5502
PubMed 15482912 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.58 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL185958 1 8.43
CHEMBL187278 1 8.30
CHEMBL184652 1 8.24
CHEMBL363275 1 7.99
CHEMBL366151 1 7.89
CHEMBL360181 1 7.81
CHEMBL425714 1 7.80
CHEMBL445652 1 7.75
CHEMBL183203 1 7.70
CHEMBL184640 1 7.64
CHEMBL188182 1 7.60
CHEMBL185850 1 7.60
CHEMBL186585 1 7.57
CHEMBL184671 1 7.38
CHEMBL360642 1 7.36
CHEMBL359967 1 7.34
CHEMBL185672 1 7.24
CHEMBL184066 1 7.01
CHEMBL184884 1 6.85
CHEMBL364351 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL185958 Ki = 3.7 nM 8.43
CHEMBL187278 Ki = 5.0 nM 8.30
CHEMBL184652 Ki = 5.7 nM 8.24
CHEMBL363275 Ki = 10.3 nM 7.99
CHEMBL366151 Ki = 13.0 nM 7.89
CHEMBL360181 Ki = 15.5 nM 7.81
CHEMBL425714 Ki = 16.0 nM 7.80
CHEMBL445652 Ki = 18.0 nM 7.75
CHEMBL183203 Ki = 20.0 nM 7.70
CHEMBL184640 Ki = 23.0 nM 7.64
CHEMBL188182 Ki = 25.0 nM 7.60
CHEMBL185850 Ki = 25.0 nM 7.60
CHEMBL186585 Ki = 27.0 nM 7.57
CHEMBL184671 Ki = 42.0 nM 7.38
CHEMBL360642 Ki = 44.0 nM 7.36
CHEMBL359967 Ki = 46.0 nM 7.34
CHEMBL185672 Ki = 57.0 nM 7.24
CHEMBL184066 Ki = 98.0 nM 7.01
CHEMBL184884 Ki = 141.0 nM 6.85
CHEMBL364351 Ki = 1011.0 nM 6.00