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Assay Detail

CHEMBL619047

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

Binding
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 4 (CHEMBL4317)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Arylcarbamate derivatives of 1-piperidineethanol as potent ligands for 5-HT4 receptors.
Soulier JL, Yang D, Brémont B, Croci T, Guzzi U, Langlois M.
J Med Chem (1997) 40 : 1755 -1761
PubMed 9171886 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 8.16 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL33884 1 9.82
CHEMBL50660 1 9.59
CHEMBL48836 1 8.98
CHEMBL286136 1 8.97
CHEMBL2115017 1 8.94
CHEMBL48684 1 8.59
CHEMBL298920 1 8.59
CHEMBL301510 1 8.38
CHEMBL287045 1 8.26
CHEMBL51251 1 8.05
CHEMBL48351 1 7.50
CHEMBL300476 1 7.22
CHEMBL301967 1 7.09
CHEMBL51647 1 6.33
CHEMBL49907 1 6.14
CHEMBL440670 1 -
CHEMBL51218 1 -
CHEMBL52167 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL33884 Ki = 0.15 nM 9.82
CHEMBL50660 Ki = 0.26 nM 9.59
CHEMBL48836 Ki = 1.05 nM 8.98
CHEMBL286136 Ki = 1.07 nM 8.97
CHEMBL2115017 Ki = 1.16 nM 8.94
CHEMBL48684 Ki = 2.6 nM 8.59
CHEMBL298920 Ki = 2.6 nM 8.59
CHEMBL301510 Ki = 4.2 nM 8.38
CHEMBL287045 Ki = 5.5 nM 8.26
CHEMBL51251 Ki = 8.9 nM 8.05
CHEMBL48351 Ki = 31.7 nM 7.50
CHEMBL300476 Ki = 60.8 nM 7.22
CHEMBL301967 Ki = 81.0 nM 7.09
CHEMBL51647 Ki = 469.0 nM 6.33
CHEMBL49907 Ki = 728.0 nM 6.14
CHEMBL440670 Ki > 1000.0 nM -
CHEMBL51218 Ki > 1000.0 nM -
CHEMBL52167 Ki > 1000.0 nM -