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Assay Detail

CHEMBL619041

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

Binding
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Striatum
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Design of a potent 5-HT4 receptor agonist with nanomolar affinity
Langlois M, Zhang L, Bre mont B, Shen S, Manara L, Croci T
Bioorg Med Chem Lett (1994) 4 : 1433 -1436
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.30 8.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL286136 1 8.97
CHEMBL287045 1 8.28
CHEMBL33732 1 7.99
CHEMBL34224 1 7.64
CHEMBL32986 1 7.46
CHEMBL33676 1 7.19
CHEMBL288199 1 7.04
CHEMBL41769 1 6.31
CHEMBL18041 ZACOPRIDE 2.0 1 6.12
CHEMBL86 METOCLOPRAMIDE 4.0 1 6.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL286136 Ki = 1.07 nM 8.97
CHEMBL287045 Ki = 5.3 nM 8.28
CHEMBL33732 Ki = 10.3 nM 7.99
CHEMBL34224 Ki = 23.0 nM 7.64
CHEMBL32986 Ki = 34.5 nM 7.46
CHEMBL33676 Ki = 64.3 nM 7.19
CHEMBL288199 Ki = 91.4 nM 7.04
CHEMBL41769 Ki = 488.0 nM 6.31
CHEMBL18041 ZACOPRIDE Ki = 753.0 nM 6.12
CHEMBL86 METOCLOPRAMIDE Ki = 975.0 nM 6.01