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Assay Detail

CHEMBL3367331

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

Binding
Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery and pharmacological profile of new hydrophilic 5-HT(4) receptor antagonists.
Brudeli B, Navaratnarajah M, Andressen KW, Manfra O, Moltzau LR, Nilsen NO, Levy FO, Klaveness J.
Bioorg Med Chem Lett (2014) 24 : 4598 -4602
PubMed 25149506 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 9.06 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3329805 1 10.30
CHEMBL3329814 1 10.10
CHEMBL3329803 1 9.70
CHEMBL3329806 1 9.70
CHEMBL3329807 1 9.70
CHEMBL3329809 1 9.70
CHEMBL33884 1 9.60
CHEMBL3329808 1 9.60
CHEMBL3329813 1 9.50
CHEMBL356359 PIBOSEROD 2.0 1 9.40
CHEMBL3329804 1 9.00
CHEMBL3329810 1 8.90
CHEMBL3329811 1 8.90
CHEMBL3329812 1 8.90
CHEMBL3329226 1 8.80
CHEMBL3329801 1 6.30
CHEMBL3329802 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3329805 Ki = 0.05012 nM 10.30
CHEMBL3329814 Ki = 0.07943 nM 10.10
CHEMBL3329803 Ki = 0.1995 nM 9.70
CHEMBL3329806 Ki = 0.1995 nM 9.70
CHEMBL3329807 Ki = 0.1995 nM 9.70
CHEMBL3329809 Ki = 0.1995 nM 9.70
CHEMBL33884 Ki = 0.2512 nM 9.60
CHEMBL3329808 Ki = 0.2512 nM 9.60
CHEMBL3329813 Ki = 0.3162 nM 9.50
CHEMBL356359 PIBOSEROD Ki = 0.3981 nM 9.40
CHEMBL3329804 Ki = 1.0 nM 9.00
CHEMBL3329810 Ki = 1.259 nM 8.90
CHEMBL3329811 Ki = 1.259 nM 8.90
CHEMBL3329812 Ki = 1.259 nM 8.90
CHEMBL3329226 Ki = 1.585 nM 8.80
CHEMBL3329801 Ki = 501.19 nM 6.30
CHEMBL3329802 Ki = 1000.0 nM 6.00