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Assay Detail

CHEMBL3594589

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Functional
Agonist activity at human 5-HT1A receptor expressed in human HeLa cell membranes assessed as stimulation of [35S]GTPgammaS binding after 20 mins by liquid scintillation counting analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

Arylpiperazine agonists of the serotonin 5-HT1A receptor preferentially activate cAMP signaling versus recruitment of β-arrestin-2.
Stroth N, Niso M, Colabufo NA, Perrone R, Svenningsson P, Lacivita E, Leopoldo M.
Bioorg Med Chem (2015) 23 : 4824 -4830
PubMed 26081758 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 9.37 10.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL511857 1 10.55
CHEMBL423181 1 9.80
CHEMBL140406 1 9.51
CHEMBL139505 1 9.42
CHEMBL444590 1 9.32
CHEMBL344146 1 7.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL511857 Ki = 0.028 nM 10.55
CHEMBL423181 Ki = 0.16 nM 9.80
CHEMBL140406 Ki = 0.31 nM 9.51
CHEMBL139505 Ki = 0.38 nM 9.42
CHEMBL444590 Ki = 0.48 nM 9.32
CHEMBL344146 Ki = 23.0 nM 7.64