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Assay Detail

CHEMBL619043

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

Binding
Binding affinity to 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum membrane
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Benzimidazole derivatives. 3. 3D-QSAR/CoMFA model and computational simulation for the recognition of 5-HT(4) receptor antagonists.
López-Rodríguez ML, Murcia M, Benhamú B, Viso A, Campillo M, Pardo L.
J Med Chem (2002) 45 : 4806 -4815
PubMed 12383006 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 8.01 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL329487 1 9.96
CHEMBL262950 1 9.54
CHEMBL94880 1 9.49
CHEMBL97955 1 9.27
CHEMBL95178 1 9.19
CHEMBL97594 1 8.66
CHEMBL94784 1 8.64
CHEMBL316856 1 8.54
CHEMBL327192 1 7.94
CHEMBL98734 1 7.86
CHEMBL97591 1 7.65
CHEMBL94756 1 7.61
CHEMBL94099 1 7.58
CHEMBL319663 1 7.56
CHEMBL98397 1 7.35
CHEMBL329545 1 7.32
CHEMBL18769 1 7.27
CHEMBL314299 1 7.16
CHEMBL96667 1 6.94
CHEMBL94415 1 6.54
CHEMBL18473 1 6.14
CHEMBL279823 1 -
CHEMBL420638 1 -
CHEMBL330605 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL329487 Ki = 0.11 nM 9.96
CHEMBL262950 Ki = 0.29 nM 9.54
CHEMBL94880 Ki = 0.32 nM 9.49
CHEMBL97955 Ki = 0.54 nM 9.27
CHEMBL95178 Ki = 0.64 nM 9.19
CHEMBL97594 Ki = 2.2 nM 8.66
CHEMBL94784 Ki = 2.3 nM 8.64
CHEMBL316856 Ki = 2.9 nM 8.54
CHEMBL327192 Ki = 11.4 nM 7.94
CHEMBL98734 Ki = 13.7 nM 7.86
CHEMBL97591 Ki = 22.4 nM 7.65
CHEMBL94756 Ki = 24.6 nM 7.61
CHEMBL94099 Ki = 26.1 nM 7.58
CHEMBL319663 Ki = 27.8 nM 7.56
CHEMBL98397 Ki = 44.6 nM 7.35
CHEMBL329545 Ki = 48.2 nM 7.32
CHEMBL18769 Ki = 54.0 nM 7.27
CHEMBL314299 Ki = 69.2 nM 7.16
CHEMBL96667 Ki = 115.0 nM 6.94
CHEMBL94415 Ki = 290.0 nM 6.54
CHEMBL18473 Ki = 719.0 nM 6.14
CHEMBL279823 Ki > 10000.0 nM -
CHEMBL420638 Ki > 1000.0 nM -
CHEMBL330605 Ki > 1000.0 nM -