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Assay Detail

CHEMBL3596033

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Binding
Agonist activity at human 5-HT1A receptor expressed in CHO cells after 90 mins by beta-arrestin-2 recruitment assay
8
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
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
EC50 5 7.49 9.49
pEC50 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL511857 1 9.49
CHEMBL423181 1 8.45
CHEMBL56 8-OH-DPAT 1 7.29
CHEMBL39 SEROTONIN 3.0 1 6.77
CHEMBL140406 1 5.47
CHEMBL444590 1 -
CHEMBL139505 1 -
CHEMBL344146 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL511857 EC50 = 0.3236 nM 9.49
CHEMBL423181 EC50 = 3.548 nM 8.45
CHEMBL56 8-OH-DPAT EC50 = 51.29 nM 7.29
CHEMBL39 SEROTONIN EC50 = 169.82 nM 6.77
CHEMBL140406 EC50 = 3388.44 nM 5.47
CHEMBL444590 pEC50 - -
CHEMBL139505 pEC50 - -
CHEMBL344146 pEC50 - -