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Assay Detail

CHEMBL2404386

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Functional
Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

Discovery of TD-8954, a clinical stage 5-HT(4) receptor agonist with gastrointestinal prokinetic properties.
McKinnell RM, Armstrong SR, Beattie DT, Fatheree PR, Long DD, Marquess DG, Shaw JP, Vickery RG.
Bioorg Med Chem Lett (2013) 23 : 4210 -4215
PubMed 23756062 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 8.54 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2402900 1 9.40
CHEMBL2402904 FELCISETRAG 2.0 1 9.30
CHEMBL2402891 1 9.20
CHEMBL2402892 1 9.20
CHEMBL2402894 1 9.10
CHEMBL2402897 1 9.10
CHEMBL2402903 1 9.00
CHEMBL2402890 1 9.00
CHEMBL2401750 1 8.80
CHEMBL2402902 1 8.80
CHEMBL2402895 1 8.80
CHEMBL2402898 1 8.80
CHEMBL2402901 1 8.70
CHEMBL76370 TEGASEROD 4.0 1 8.60
CHEMBL2402899 1 8.50
CHEMBL2402893 1 8.50
CHEMBL2402887 1 8.00
CHEMBL1729 CISAPRIDE 4.0 1 7.10
CHEMBL2402888 1 6.60
CHEMBL2402889 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2402900 EC50 = 0.3981 nM 9.40
CHEMBL2402904 FELCISETRAG EC50 = 0.5012 nM 9.30
CHEMBL2402891 EC50 = 0.631 nM 9.20
CHEMBL2402892 EC50 = 0.631 nM 9.20
CHEMBL2402894 EC50 = 0.7943 nM 9.10
CHEMBL2402897 EC50 = 0.7943 nM 9.10
CHEMBL2402903 EC50 = 1.0 nM 9.00
CHEMBL2402890 EC50 = 1.0 nM 9.00
CHEMBL2401750 EC50 = 1.585 nM 8.80
CHEMBL2402902 EC50 = 1.585 nM 8.80
CHEMBL2402895 EC50 = 1.585 nM 8.80
CHEMBL2402898 EC50 = 1.585 nM 8.80
CHEMBL2402901 EC50 = 1.995 nM 8.70
CHEMBL76370 TEGASEROD EC50 = 2.512 nM 8.60
CHEMBL2402899 EC50 = 3.162 nM 8.50
CHEMBL2402893 EC50 = 3.162 nM 8.50
CHEMBL2402887 EC50 = 10.0 nM 8.00
CHEMBL1729 CISAPRIDE EC50 = 79.43 nM 7.10
CHEMBL2402888 EC50 = 251.19 nM 6.60
CHEMBL2402889 EC50 = 630.96 nM 6.20