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Assay Detail

CHEMBL884801

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

Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
75
Total Activities
73
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

Conformationally constrained N1-arylsulfonyltryptamine derivatives as 5-HT6 receptor antagonists.
Cole DC, Lennox WJ, Stock JR, Ellingboe JW, Mazandarani H, Smith DL, Zhang G, Tawa GJ, Schechter LE.
Bioorg Med Chem Lett (2005) 15 : 4780 -4785
PubMed 16125933 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 75 8.00 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL371292 3 9.00
CHEMBL370507 1 9.00
CHEMBL365774 1 9.00
CHEMBL193450 1 9.00
CHEMBL194590 1 9.00
CHEMBL425196 1 9.00
CHEMBL372364 1 8.82
CHEMBL179592 1 8.70
CHEMBL196692 1 8.70
CHEMBL193358 1 8.70
CHEMBL76237 1 8.64
CHEMBL198827 1 8.52
CHEMBL196466 1 8.52
CHEMBL383373 1 8.52
CHEMBL365753 1 8.52
CHEMBL434932 1 8.52
CHEMBL371318 1 8.52
CHEMBL413525 1 8.40
CHEMBL195018 1 8.40
CHEMBL196622 1 8.40
CHEMBL193824 1 8.34
CHEMBL196619 1 8.30
CHEMBL370215 1 8.30
CHEMBL196102 1 8.30
CHEMBL363843 1 8.15
CHEMBL196094 1 8.15
CHEMBL371469 1 8.15
CHEMBL427184 1 8.15
CHEMBL197845 1 8.10
CHEMBL371886 1 8.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL371292 Ki = 1.0 nM 9.00
CHEMBL425196 Ki = 1.0 nM 9.00
CHEMBL365774 Ki = 1.0 nM 9.00
CHEMBL193450 Ki = 1.0 nM 9.00
CHEMBL370507 Ki = 1.0 nM 9.00
CHEMBL194590 Ki = 1.0 nM 9.00
CHEMBL372364 Ki = 1.5 nM 8.82
CHEMBL179592 Ki = 2.0 nM 8.70
CHEMBL196692 Ki = 2.0 nM 8.70
CHEMBL371292 Ki = 2.0 nM 8.70
CHEMBL193358 Ki = 2.0 nM 8.70
CHEMBL76237 Ki = 2.3 nM 8.64
CHEMBL371292 Ki = 3.0 nM 8.52
CHEMBL196466 Ki = 3.0 nM 8.52
CHEMBL198827 Ki = 3.0 nM 8.52
CHEMBL383373 Ki = 3.0 nM 8.52
CHEMBL371318 Ki = 3.0 nM 8.52
CHEMBL434932 Ki = 3.0 nM 8.52
CHEMBL365753 Ki = 3.0 nM 8.52
CHEMBL413525 Ki = 4.0 nM 8.40
CHEMBL195018 Ki = 4.0 nM 8.40
CHEMBL196622 Ki = 4.0 nM 8.40
CHEMBL193824 Ki = 4.6 nM 8.34
CHEMBL196102 Ki = 5.0 nM 8.30
CHEMBL196619 Ki = 5.0 nM 8.30
CHEMBL370215 Ki = 5.0 nM 8.30
CHEMBL363843 Ki = 7.0 nM 8.15
CHEMBL196094 Ki = 7.0 nM 8.15
CHEMBL371469 Ki = 7.0 nM 8.15
CHEMBL427184 Ki = 7.0 nM 8.15
CHEMBL197845 Ki = 8.0 nM 8.10
CHEMBL371886 Ki = 8.0 nM 8.10
CHEMBL194786 Ki = 8.0 nM 8.10
CHEMBL194307 Ki = 8.0 nM 8.10
CHEMBL371132 Ki = 8.5 nM 8.07
CHEMBL366012 Ki = 9.0 nM 8.05
CHEMBL363827 Ki = 9.2 nM 8.04
CHEMBL372569 Ki = 9.8 nM 8.01
CHEMBL196743 Ki = 10.0 nM 8.00
CHEMBL194750 Ki = 10.0 nM 8.00
CHEMBL194568 Ki = 10.5 nM 7.98
CHEMBL369910 Ki = 11.0 nM 7.96
CHEMBL198941 Ki = 12.0 nM 7.92
CHEMBL194904 Ki = 13.0 nM 7.89
CHEMBL196926 Ki = 13.0 nM 7.89
CHEMBL198766 Ki = 14.0 nM 7.85
CHEMBL380556 Ki = 14.0 nM 7.85
CHEMBL380772 Ki = 15.0 nM 7.82
CHEMBL196792 Ki = 16.0 nM 7.80
CHEMBL197407 Ki = 19.3 nM 7.71