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Assay Detail

CHEMBL4122688

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

Functional
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
23
Total Activities
23
Compounds Tested
1
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

Design, synthesis and evaluation of vilazodone-tacrine hybrids as multitarget-directed ligands against depression with cognitive impairment.
Liu W, Wang H, Li X, Xu Y, Zhang J, Wang W, Gong Q, Qiu X, Zhu J, Mao F, Zhang H, Li J.
Bioorg Med Chem (2018) 26 : 3117 -3125
PubMed 29729987 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 8.14 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL439849 VILAZODONE 4.0 1 9.92
CHEMBL4128200 1 9.46
CHEMBL4126644 1 9.44
CHEMBL4128689 1 9.24
CHEMBL4130230 1 9.22
CHEMBL4129170 1 9.14
CHEMBL4127774 1 9.12
CHEMBL4126818 1 8.92
CHEMBL4125762 1 8.81
CHEMBL4129917 1 7.83
CHEMBL4129051 1 7.54
CHEMBL4126486 1 7.46
CHEMBL4125732 1 7.28
CHEMBL4128838 1 7.21
CHEMBL4130176 1 7.03
CHEMBL4130059 1 6.84
CHEMBL4127877 1 6.25
CHEMBL4127445 1 5.81
CHEMBL95 TACRINE 4.0 1 -
CHEMBL395280 HUPERZINE A 2.0 1 -
CHEMBL4126958 1 -
CHEMBL4129019 1 -
CHEMBL4126912 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL439849 VILAZODONE EC50 = 0.12 nM 9.92
CHEMBL4128200 EC50 = 0.35 nM 9.46
CHEMBL4126644 EC50 = 0.36 nM 9.44
CHEMBL4128689 EC50 = 0.58 nM 9.24
CHEMBL4130230 EC50 = 0.6 nM 9.22
CHEMBL4129170 EC50 = 0.72 nM 9.14
CHEMBL4127774 EC50 = 0.75 nM 9.12
CHEMBL4126818 EC50 = 1.2 nM 8.92
CHEMBL4125762 EC50 = 1.55 nM 8.81
CHEMBL4129917 EC50 = 14.93 nM 7.83
CHEMBL4129051 EC50 = 28.8 nM 7.54
CHEMBL4126486 EC50 = 34.98 nM 7.46
CHEMBL4125732 EC50 = 52.0 nM 7.28
CHEMBL4128838 EC50 = 62.43 nM 7.21
CHEMBL4130176 EC50 = 93.37 nM 7.03
CHEMBL4130059 EC50 = 146.01 nM 6.84
CHEMBL4127877 EC50 = 567.0 nM 6.25
CHEMBL4127445 EC50 = 1563.21 nM 5.81
CHEMBL95 TACRINE EC50 - -
CHEMBL395280 HUPERZINE A EC50 - -
CHEMBL4126958 EC50 < 0.14 nM -
CHEMBL4129019 EC50 < 0.14 nM -
CHEMBL4126912 EC50 > 10000.0 nM -