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Assay Detail

CHEMBL4390417

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

Binding
Displacement of [3H]ketanserin from 5HT2A receptor in rat cortical membranes incubated for 15 mins by liquid scintillation spectrometry
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants.
Zaręba P, Jaśkowska J, Czekaj I, Satała G.
Bioorg Med Chem (2019) 27 : 3396 -3407
PubMed 31253535 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.56 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL83894 FANANSERIN 2.0 1 10.22
CHEMBL83975 1 8.52
CHEMBL82826 1 8.43
CHEMBL83035 1 8.30
CHEMBL83780 1 8.15
CHEMBL415272 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL83894 FANANSERIN Ki = 0.06 nM 10.22
CHEMBL83975 Ki = 3.0 nM 8.52
CHEMBL82826 Ki = 3.7 nM 8.43
CHEMBL83035 Ki = 5.0 nM 8.30
CHEMBL83780 Ki = 7.0 nM 8.15
CHEMBL415272 Ki = 18.0 nM 7.75