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Assay Detail

CHEMBL3878029

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

Binding
Displacement of [3H]8-OH-DPAT from recombinant human 5-HT1A receptor expressed in HeLa cell membranes after 30 mins by TopCount liquid scintillation counting method
12
Total Activities
12
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

Synthesis, biological evaluation and molecular modeling of 1-oxa-4-thiaspiro- and 1,4-dithiaspiro[4.5]decane derivatives as potent and selective 5-HT1A receptor agonists.
Franchini S, Manasieva LI, Sorbi C, Battisti UM, Fossa P, Cichero E, Denora N, Iacobazzi RM, Cilia A, Pirona L, Ronsisvalle S, Aricò G, Brasili L.
Eur J Med Chem (2017) 125 : 435 -452
PubMed 27689727 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 8.34 9.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3938383 1 9.03
CHEMBL13647 BMY-7378 1 8.90
CHEMBL3917316 1 8.81
CHEMBL3901382 1 8.65
CHEMBL3981480 1 8.52
CHEMBL3929328 1 8.52
CHEMBL3892434 1 8.30
CHEMBL2234448 1 8.29
CHEMBL3970754 1 7.64
CHEMBL1963046 1 7.64
CHEMBL1183249 1 7.43
CHEMBL3911497 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3938383 Ki = 0.9333 nM 9.03
CHEMBL13647 BMY-7378 Ki = 1.259 nM 8.90
CHEMBL3917316 Ki = 1.549 nM 8.81
CHEMBL3901382 Ki = 2.239 nM 8.65
CHEMBL3981480 Ki = 3.02 nM 8.52
CHEMBL3929328 Ki = 3.02 nM 8.52
CHEMBL3892434 Ki = 5.012 nM 8.30
CHEMBL2234448 Ki = 5.129 nM 8.29
CHEMBL3970754 Ki = 22.91 nM 7.64
CHEMBL1963046 Ki = 22.91 nM 7.64
CHEMBL1183249 Ki = 37.15 nM 7.43
CHEMBL3911497 Ki > 1000.0 nM -