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Assay Detail

CHEMBL3773936

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

Binding
Displacement of [3H]8-OH-DPAT from human 5-HT1A expressed in human HeLa cells after 30 mins
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Scouting new sigma receptor ligands: Synthesis, pharmacological evaluation and molecular modeling of 1,3-dioxolane-based structures and derivatives.
Franchini S, Battisti UM, Prandi A, Tait A, Borsari C, Cichero E, Fossa P, Cilia A, Prezzavento O, Ronsisvalle S, Aricò G, Parenti C, Brasili L.
Eur J Med Chem (2016) 112 : 1 -19
PubMed 26874044 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 7.20 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3770589 1 8.14
CHEMBL3770151 1 8.12
CHEMBL178700 1 7.75
CHEMBL3769446 1 7.30
CHEMBL359663 1 7.16
CHEMBL3771016 1 6.90
CHEMBL3769904 1 6.79
CHEMBL3770593 1 6.38
CHEMBL3770830 1 6.26
CHEMBL3770485 1 -
CHEMBL3769508 1 -
CHEMBL3769960 1 -
CHEMBL3769675 1 -
CHEMBL3769895 1 -
CHEMBL3769874 1 -
CHEMBL3770532 1 -
CHEMBL3771186 1 -
CHEMBL3770832 1 -
CHEMBL3770762 1 -
CHEMBL3770871 1 -
CHEMBL3769801 1 -
CHEMBL3770072 1 -
CHEMBL3771163 1 -
CHEMBL3770992 1 -
CHEMBL3771017 1 -
CHEMBL3770681 1 -
CHEMBL3769825 1 -
CHEMBL3769930 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3770589 Ki = 7.244 nM 8.14
CHEMBL3770151 Ki = 7.586 nM 8.12
CHEMBL178700 Ki = 17.78 nM 7.75
CHEMBL3769446 Ki = 50.12 nM 7.30
CHEMBL359663 Ki = 69.18 nM 7.16
CHEMBL3771016 Ki = 125.89 nM 6.90
CHEMBL3769904 Ki = 162.18 nM 6.79
CHEMBL3770593 Ki = 416.87 nM 6.38
CHEMBL3770830 Ki = 549.54 nM 6.26
CHEMBL3770485 Ki > 1000.0 nM -
CHEMBL3769508 Ki > 1000.0 nM -
CHEMBL3769960 Ki > 1000.0 nM -
CHEMBL3769675 Ki > 1000.0 nM -
CHEMBL3769895 Ki > 1000.0 nM -
CHEMBL3769874 Ki > 1000.0 nM -
CHEMBL3770532 Ki > 1000.0 nM -
CHEMBL3771186 Ki > 1000.0 nM -
CHEMBL3770832 Ki > 1000.0 nM -
CHEMBL3770762 Ki > 1000.0 nM -
CHEMBL3770871 Ki > 1000.0 nM -
CHEMBL3769801 Ki > 1000.0 nM -
CHEMBL3770072 Ki > 1000.0 nM -
CHEMBL3771163 Ki > 1000.0 nM -
CHEMBL3770992 Ki > 1000.0 nM -
CHEMBL3771017 Ki > 1000.0 nM -
CHEMBL3770681 Ki > 1000.0 nM -
CHEMBL3769825 Ki > 1000.0 nM -
CHEMBL3769930 Ki > 1000.0 nM -