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Assay Detail

CHEMBL616134

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Binding
Tested in vitro for its ability to bind to 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and pharmacological characterization of a series of geometrically constrained 5-HT(2A/2C) receptor ligands.
Chambers JJ, Parrish JC, Jensen NH, Kurrasch-Orbaugh DM, Marona-Lewicka D, Nichols DE.
J Med Chem (2003) 46 : 3526 -3535
PubMed 12877591 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.51 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL263881 LYSERGIDE 2.0 1 8.96
CHEMBL116940 1 6.98
CHEMBL119323 1 6.28
CHEMBL331864 1 6.26
CHEMBL119584 1 6.07
CHEMBL445106 1 6.02
CHEMBL117689 1 6.00
CHEMBL116209 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL263881 LYSERGIDE Ki = 1.1 nM 8.96
CHEMBL116940 Ki = 105.0 nM 6.98
CHEMBL119323 Ki = 520.0 nM 6.28
CHEMBL331864 Ki = 550.0 nM 6.26
CHEMBL119584 Ki = 860.0 nM 6.07
CHEMBL445106 Ki = 960.0 nM 6.02
CHEMBL117689 Ki = 1000.0 nM 6.00
CHEMBL116209 Ki = 3000.0 nM 5.52