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Assay Detail

CHEMBL805830

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

Binding
In vitro binding affinity towards serotonin 5-HT2A receptor in rat cortical membranes using [3H]ketanserin as radioligand
20
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2A (CHEMBL322)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

1,1-diphenyl-3-dialkylamino-1-silacyclopentane derivatives: A new class of potent and selective 5-HT2A antagonists
Damour D, Barreau M, Dutruc-Rosset G, Doble A, Piot O, Mignani S
Bioorg Med Chem Lett (1994) 4 : 415 -420
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.91 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL337226 1 9.05
CHEMBL133104 1 9.00
CHEMBL267777 RITANSERIN 2.0 1 8.77
CHEMBL134423 4 8.70
CHEMBL135898 1 8.47
CHEMBL134351 1 8.00
CHEMBL134502 1 7.85
CHEMBL134964 1 7.75
CHEMBL134394 2 7.70
CHEMBL335615 1 7.60
CHEMBL134804 1 7.54
CHEMBL335616 1 7.48
CHEMBL133430 1 7.34
CHEMBL335029 1 7.28
CHEMBL134065 1 7.10
CHEMBL336401 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL337226 IC50 = 0.9 nM 9.05
CHEMBL133104 IC50 = 1.0 nM 9.00
CHEMBL267777 RITANSERIN IC50 = 1.7 nM 8.77
CHEMBL134423 IC50 = 2.0 nM 8.70
CHEMBL134423 IC50 = 3.0 nM 8.52
CHEMBL135898 IC50 = 3.4 nM 8.47
CHEMBL134351 IC50 = 10.0 nM 8.00
CHEMBL134502 IC50 = 14.0 nM 7.85
CHEMBL134423 IC50 = 16.0 nM 7.80
CHEMBL134964 IC50 = 18.0 nM 7.75
CHEMBL134394 IC50 = 20.0 nM 7.70
CHEMBL335615 IC50 = 25.0 nM 7.60
CHEMBL134423 IC50 = 25.0 nM 7.60
CHEMBL134394 IC50 = 27.0 nM 7.57
CHEMBL134804 IC50 = 29.0 nM 7.54
CHEMBL335616 IC50 = 33.0 nM 7.48
CHEMBL133430 IC50 = 46.0 nM 7.34
CHEMBL335029 IC50 = 53.0 nM 7.28
CHEMBL134065 IC50 = 80.0 nM 7.10
CHEMBL336401 IC50 = 100.0 nM 7.00