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Assay Detail

CHEMBL3222890

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

Binding
Antagonist activity at 5TH4 receptor (unknown origin)
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

SAR mining and its application to the design of TRPA1 antagonists
Mills JEJ, Brown AD, Ryckmans T, Miller DC, Skerratt SE, Barker CM, Bunnage ME
Medchemcomm (2012) 3 : 174 -178
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.44 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3220223 1 8.85
CHEMBL334325 1 8.52
CHEMBL421256 1 7.77
CHEMBL339936 1 7.75
CHEMBL121766 1 7.19
CHEMBL127876 1 6.79
CHEMBL125670 1 6.53
CHEMBL124485 1 6.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3220223 IC50 = 1.4 nM 8.85
CHEMBL334325 IC50 = 3.0 nM 8.52
CHEMBL421256 IC50 = 17.0 nM 7.77
CHEMBL339936 IC50 = 18.0 nM 7.75
CHEMBL121766 IC50 = 64.0 nM 7.19
CHEMBL127876 IC50 = 162.0 nM 6.79
CHEMBL125670 IC50 = 296.0 nM 6.53
CHEMBL124485 IC50 = 715.0 nM 6.15