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Assay Detail

CHEMBL856238

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

Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
IC50 29 7.58 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL194307 1 9.22
CHEMBL371886 1 9.10
CHEMBL413525 1 9.00
CHEMBL194750 1 8.14
CHEMBL198941 1 8.14
CHEMBL427184 1 8.12
CHEMBL196094 1 8.09
CHEMBL369910 1 7.96
CHEMBL194590 1 7.81
CHEMBL380556 1 7.68
CHEMBL383373 1 7.61
CHEMBL370507 1 7.60
CHEMBL193450 1 7.36
CHEMBL198827 1 7.30
CHEMBL193358 1 7.28
CHEMBL425196 1 7.27
CHEMBL370215 1 7.25
CHEMBL380772 1 7.21
CHEMBL371469 1 7.12
CHEMBL196102 1 7.09
CHEMBL365774 1 7.07
CHEMBL195018 1 7.02
CHEMBL196619 1 7.01
CHEMBL365753 1 6.97
CHEMBL196466 1 6.96
CHEMBL366012 1 6.96
CHEMBL434932 1 6.95
CHEMBL194786 1 6.91
CHEMBL371292 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL194307 IC50 = 0.6 nM 9.22
CHEMBL371886 IC50 = 0.8 nM 9.10
CHEMBL413525 IC50 = 1.0 nM 9.00
CHEMBL194750 IC50 = 7.3 nM 8.14
CHEMBL198941 IC50 = 7.3 nM 8.14
CHEMBL427184 IC50 = 7.6 nM 8.12
CHEMBL196094 IC50 = 8.2 nM 8.09
CHEMBL369910 IC50 = 11.0 nM 7.96
CHEMBL194590 IC50 = 15.5 nM 7.81
CHEMBL380556 IC50 = 21.0 nM 7.68
CHEMBL383373 IC50 = 24.5 nM 7.61
CHEMBL370507 IC50 = 25.0 nM 7.60
CHEMBL193450 IC50 = 43.6 nM 7.36
CHEMBL198827 IC50 = 49.5 nM 7.30
CHEMBL193358 IC50 = 52.5 nM 7.28
CHEMBL425196 IC50 = 53.3 nM 7.27
CHEMBL370215 IC50 = 56.3 nM 7.25
CHEMBL380772 IC50 = 61.0 nM 7.21
CHEMBL371469 IC50 = 76.5 nM 7.12
CHEMBL196102 IC50 = 81.4 nM 7.09
CHEMBL365774 IC50 = 85.5 nM 7.07
CHEMBL195018 IC50 = 96.2 nM 7.02
CHEMBL196619 IC50 = 96.7 nM 7.01
CHEMBL365753 IC50 = 107.1 nM 6.97
CHEMBL196466 IC50 = 110.0 nM 6.96
CHEMBL366012 IC50 = 110.0 nM 6.96
CHEMBL434932 IC50 = 112.0 nM 6.95
CHEMBL194786 IC50 = 123.0 nM 6.91
CHEMBL371292 IC50 = - nM -