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Assay Detail

CHEMBL620705

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

Binding
Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type C6
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Synthesis and characterization of the first fluorescent antagonists for human 5-HT4 receptors.
Berque-Bestel I, Soulier JL, Giner M, Rivail L, Langlois M, Sicsic S.
J Med Chem (2003) 46 : 2606 -2620
PubMed 12801225 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.25 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL286136 1 9.00
CHEMBL328918 1 8.15
CHEMBL89225 1 8.12
CHEMBL315590 1 7.62
CHEMBL86777 1 7.51
CHEMBL327999 1 7.50
CHEMBL88355 1 7.23
CHEMBL85125 1 7.19
CHEMBL90559 1 7.11
CHEMBL315526 1 7.02
CHEMBL86985 1 6.94
CHEMBL86624 1 6.75
CHEMBL156206 1 6.74
CHEMBL87063 1 6.74
CHEMBL433149 1 6.58
CHEMBL312940 1 5.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL286136 Ki = 1.0 nM 9.00
CHEMBL328918 Ki = 7.0 nM 8.15
CHEMBL89225 Ki = 7.5 nM 8.12
CHEMBL315590 Ki = 24.0 nM 7.62
CHEMBL86777 Ki = 31.0 nM 7.51
CHEMBL327999 Ki = 32.0 nM 7.50
CHEMBL88355 Ki = 59.0 nM 7.23
CHEMBL85125 Ki = 64.0 nM 7.19
CHEMBL90559 Ki = 77.0 nM 7.11
CHEMBL315526 Ki = 96.0 nM 7.02
CHEMBL86985 Ki = 116.0 nM 6.94
CHEMBL86624 Ki = 180.0 nM 6.75
CHEMBL156206 Ki = 183.0 nM 6.74
CHEMBL87063 Ki = 181.0 nM 6.74
CHEMBL433149 Ki = 264.0 nM 6.58
CHEMBL312940 Ki = 1720.0 nM 5.76