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Assay Detail

CHEMBL5047396

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 incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
57
Total Activities
57
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

The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression.
Li X, Li J, Huang Y, Gong Q, Fu Y, Xu Y, Huang J, You H, Zhang D, Zhang D, Mao F, Zhu J, Wang H, Zhang H, Li J.
Eur J Med Chem (2022) 229 : 114045 -114045
PubMed 34922191 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 57 7.17 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL439849 VILAZODONE 4.0 1 9.10
CHEMBL56 8-OH-DPAT 1 8.48
CHEMBL5087461 1 8.07
CHEMBL5079986 1 8.05
CHEMBL5089691 1 8.04
CHEMBL5078724 1 7.75
CHEMBL5080308 1 7.72
CHEMBL5088919 1 7.66
CHEMBL5080984 1 7.65
CHEMBL5087351 1 7.65
CHEMBL5087427 1 7.60
CHEMBL5094829 1 7.58
CHEMBL5085893 1 7.58
CHEMBL5082360 1 7.55
CHEMBL5092455 1 7.54
CHEMBL5084736 1 7.54
CHEMBL5077564 1 7.51
CHEMBL5076629 1 7.44
CHEMBL5088366 1 7.30
CHEMBL5071558 1 7.24
CHEMBL5082250 1 7.23
CHEMBL5072039 1 7.18
CHEMBL5082836 1 7.18
CHEMBL5088143 1 7.18
CHEMBL5093872 1 7.00
CHEMBL5092918 1 6.97
CHEMBL5088314 1 6.91
CHEMBL5070726 1 6.91
CHEMBL5089630 1 6.79
CHEMBL5086036 1 6.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL439849 VILAZODONE EC50 = 0.79 nM 9.10
CHEMBL56 8-OH-DPAT EC50 = 3.3 nM 8.48
CHEMBL5087461 EC50 = 8.6 nM 8.07
CHEMBL5079986 EC50 = 9.0 nM 8.05
CHEMBL5089691 EC50 = 9.1 nM 8.04
CHEMBL5078724 EC50 = 17.92 nM 7.75
CHEMBL5080308 EC50 = 19.0 nM 7.72
CHEMBL5088919 EC50 = 22.0 nM 7.66
CHEMBL5080984 EC50 = 22.2 nM 7.65
CHEMBL5087351 EC50 = 22.4 nM 7.65
CHEMBL5087427 EC50 = 25.0 nM 7.60
CHEMBL5094829 EC50 = 26.0 nM 7.58
CHEMBL5085893 EC50 = 26.0 nM 7.58
CHEMBL5082360 EC50 = 28.3 nM 7.55
CHEMBL5084736 EC50 = 29.0 nM 7.54
CHEMBL5092455 EC50 = 29.0 nM 7.54
CHEMBL5077564 EC50 = 31.0 nM 7.51
CHEMBL5076629 EC50 = 36.0 nM 7.44
CHEMBL5088366 EC50 = 49.82 nM 7.30
CHEMBL5071558 EC50 = 57.0 nM 7.24
CHEMBL5082250 EC50 = 58.6 nM 7.23
CHEMBL5072039 EC50 = 65.24 nM 7.18
CHEMBL5082836 EC50 = 65.53 nM 7.18
CHEMBL5088143 EC50 = 66.6 nM 7.18
CHEMBL5093872 EC50 = 99.61 nM 7.00
CHEMBL5092918 EC50 = 106.6 nM 6.97
CHEMBL5070726 EC50 = 123.0 nM 6.91
CHEMBL5088314 EC50 = 123.78 nM 6.91
CHEMBL5089630 EC50 = 161.74 nM 6.79
CHEMBL5086036 EC50 = 160.5 nM 6.79
CHEMBL5085109 EC50 = 169.0 nM 6.77
CHEMBL5082850 EC50 = 175.6 nM 6.75
CHEMBL5087922 EC50 = 184.0 nM 6.74
CHEMBL5074796 EC50 = 202.54 nM 6.69
CHEMBL5090651 EC50 = 210.0 nM 6.68
CHEMBL5088060 EC50 = 278.8 nM 6.55
CHEMBL5089999 EC50 = 316.0 nM 6.50
CHEMBL5086277 EC50 = 323.46 nM 6.49
CHEMBL5076277 EC50 = 334.0 nM 6.48
CHEMBL5087878 EC50 = 405.0 nM 6.39
CHEMBL5078629 EC50 = 467.0 nM 6.33
CHEMBL5069928 EC50 = 521.0 nM 6.28
CHEMBL5072034 EC50 = 547.0 nM 6.26
CHEMBL5071820 EC50 = 619.88 nM 6.21
CHEMBL5091978 EC50 = 653.0 nM 6.18
CHEMBL5080825 EC50 > 1000.0 nM -
CHEMBL5087923 EC50 > 1000.0 nM -
CHEMBL5075295 EC50 > 1000.0 nM -
CHEMBL5076406 EC50 > 1000.0 nM -
CHEMBL5086121 EC50 > 1000.0 nM -