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Assay Detail

CHEMBL5362786

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

Functional
Agonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 mins
12
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of novel arylpiperazine-based DA/5-HT modulators as potential antipsychotic agents - Design, synthesis, structural studies and pharmacological profiling.
Stępnicki P, Targowska-Duda KM, Martínez AL, Zięba A, Wronikowska-Denysiuk O, Wróbel MZ, Bartyzel A, Trzpil A, Wróbel TM, Chodkowski A, Mirecka K, Karcz T, Szczepańska K, Loza MI, Budzyńska B, Turło J, Handzlik J, Fornal E, Poleszak E, Castro M, Kaczor AA.
Eur J Med Chem (2023) 252 : 115285 -115285
PubMed 37027998 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 7.97 9.57
pEC50 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18840 2 9.57
CHEMBL5409227 2 7.55
CHEMBL5431642 2 6.80
CHEMBL5418283 2 -
CHEMBL54 HALOPERIDOL 4.0 2 -
CHEMBL85 RISPERIDONE 4.0 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18840 EC50 = 0.2692 nM 9.57
CHEMBL18840 EC50 = 0.27 nM 9.57
CHEMBL5409227 EC50 = 28.18 nM 7.55
CHEMBL5409227 EC50 = 28.4 nM 7.55
CHEMBL5431642 EC50 = 158.49 nM 6.80
CHEMBL5431642 EC50 = 160.0 nM 6.80
CHEMBL5418283 pEC50 - -
CHEMBL5418283 EC50 - -
CHEMBL54 HALOPERIDOL pEC50 - -
CHEMBL54 HALOPERIDOL EC50 - -
CHEMBL85 RISPERIDONE pEC50 - -
CHEMBL85 RISPERIDONE EC50 - -