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Assay Detail

CHEMBL620706

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

Binding
Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type C6
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 4 (CHEMBL1875)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New arylpiperazine derivatives as antagonists of the human cloned 5-HT(4) receptor isoforms.
Curtet S, Soulier JL, Zahradnik I, Giner M, Berque-Bestel I, Mialet J, Lezoualc'h F, Donzeau-Gouge P, Sicsic S, Fischmeister R, Langlois M.
J Med Chem (2000) 43 : 3761 -3769
PubMed 11020291 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 7.92 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL33884 1 10.00
CHEMBL121913 1 9.00
CHEMBL331396 1 8.85
CHEMBL121776 1 8.85
CHEMBL332553 1 8.82
CHEMBL330848 1 8.70
CHEMBL334325 1 8.52
CHEMBL122914 1 8.46
CHEMBL286136 1 8.25
CHEMBL125926 1 8.04
CHEMBL125716 1 8.01
CHEMBL2112621 1 7.94
CHEMBL123377 1 7.84
CHEMBL421256 1 7.78
CHEMBL339936 1 7.75
CHEMBL122818 1 7.64
CHEMBL333028 1 7.64
CHEMBL121766 1 7.19
CHEMBL127876 1 6.79
CHEMBL331264 1 6.70
CHEMBL420166 1 6.62
CHEMBL125670 1 6.53
CHEMBL124485 1 6.15
CHEMBL125005 1 -
CHEMBL338136 1 -
CHEMBL122973 1 -
CHEMBL126098 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL33884 Ki = 0.1 nM 10.00
CHEMBL121913 Ki = 1.0 nM 9.00
CHEMBL331396 Ki = 1.4 nM 8.85
CHEMBL121776 Ki = 1.4 nM 8.85
CHEMBL332553 Ki = 1.5 nM 8.82
CHEMBL330848 Ki = 2.0 nM 8.70
CHEMBL334325 Ki = 3.0 nM 8.52
CHEMBL122914 Ki = 3.5 nM 8.46
CHEMBL286136 Ki = 5.6 nM 8.25
CHEMBL125926 Ki = 9.2 nM 8.04
CHEMBL125716 Ki = 9.8 nM 8.01
CHEMBL2112621 Ki = 11.5 nM 7.94
CHEMBL123377 Ki = 14.3 nM 7.84
CHEMBL421256 Ki = 16.8 nM 7.78
CHEMBL339936 Ki = 17.7 nM 7.75
CHEMBL122818 Ki = 23.0 nM 7.64
CHEMBL333028 Ki = 23.1 nM 7.64
CHEMBL121766 Ki = 64.0 nM 7.19
CHEMBL127876 Ki = 162.0 nM 6.79
CHEMBL331264 Ki = 199.2 nM 6.70
CHEMBL420166 Ki = 240.0 nM 6.62
CHEMBL125670 Ki = 296.0 nM 6.53
CHEMBL124485 Ki = 715.0 nM 6.15
CHEMBL125005 Ki > 1000.0 nM -
CHEMBL338136 Ki > 1000.0 nM -
CHEMBL122973 Ki > 1000.0 nM -
CHEMBL126098 Ki > 1000.0 nM -