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Assay Detail

CHEMBL1786288

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

Binding
Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in EBNA gene-positive HEK293 cells after 120 mins
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293-EBNA
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Development of Fluorescent Ligands for the Human 5-HT1A Receptor.
Alonso D, Vázquez-Villa H, Gamo AM, Martínez-Esperón MF, Tortosa M, Viso A, Fernández de la Pradilla R, Junquera E, Aicart E, Martín-Fontecha M, Benhamú B, López-Rodríguez ML, Ortega-Gutiérrez S.
ACS Med Chem Lett (2010) 1 : 249 -253
PubMed 24900203 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 8.00 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1784931 1 8.70
CHEMBL33150 1 8.62
CHEMBL1784939 1 8.62
CHEMBL1784933 1 8.30
CHEMBL42810 1 8.26
CHEMBL1784934 1 8.15
CHEMBL1784935 1 8.05
CHEMBL1784930 1 7.96
CHEMBL1784932 1 7.82
CHEMBL1784938 1 7.01
CHEMBL1784937 1 6.46
CHEMBL1784936 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1784931 Ki = 2.0 nM 8.70
CHEMBL33150 Ki = 2.4 nM 8.62
CHEMBL1784939 Ki = 2.4 nM 8.62
CHEMBL1784933 Ki = 5.0 nM 8.30
CHEMBL42810 Ki = 5.5 nM 8.26
CHEMBL1784934 Ki = 7.0 nM 8.15
CHEMBL1784935 Ki = 9.0 nM 8.05
CHEMBL1784930 Ki = 11.0 nM 7.96
CHEMBL1784932 Ki = 15.0 nM 7.82
CHEMBL1784938 Ki = 98.0 nM 7.01
CHEMBL1784937 Ki = 350.0 nM 6.46
CHEMBL1784936 Ki > 1000.0 nM -