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Assay Detail

CHEMBL896288

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Functional
Antagonist activity at human 5HT3A receptor expressed in HEK293 cells by FMP assay
ChEMBL ↗
48
Total Activities
26
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 Intermediate

Target

5-hydroxytryptamine receptor 3A (CHEMBL1899) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor.
Jensen AA, Zlotos DP, Liljefors T.
J Med Chem (2007) 50 : 4616 -4629
PubMed 17722904 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 43 4.63 5.60
EC50 5 6.32 6.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39 SEROTONIN 3.0 2 6.34
CHEMBL388048 — — 2 5.60
CHEMBL231056 — — 2 5.40
CHEMBL415568 — — 2 5.40
CHEMBL388212 — — 2 4.96
CHEMBL388046 — — 2 4.52
CHEMBL395727 — — 2 4.52
CHEMBL244561 — — 2 4.52
CHEMBL389120 — — 2 4.52
CHEMBL388049 — — 2 4.52
CHEMBL415570 — — 2 4.52
CHEMBL415569 — — 2 4.52
CHEMBL229999 — — 2 4.52
CHEMBL396705 — — 2 4.00
CHEMBL390135 — — 2 4.00
CHEMBL230952 — — 2 4.00
CHEMBL773 GLYCINE 4.0 1 -
CHEMBL96 GAMMA-AMINOBUTYRIC ACID 1.0 1 -
CHEMBL1180293 — — 2 -
CHEMBL667 ACETYLCHOLINE 4.0 1 -
CHEMBL231047 TOXIFERINE — 2 -
CHEMBL395960 — — 2 -
CHEMBL206666 — — 2 -
CHEMBL382243 — — 2 -
CHEMBL510275 METHYLLYCACONITINE — 1 -
CHEMBL229998 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39 SEROTONIN EC50 = 457.09 nM 6.34
CHEMBL39 SEROTONIN EC50 = 500.0 nM 6.30
CHEMBL388048 — IC50 = 2500.0 nM 5.60
CHEMBL388048 — IC50 = 2511.89 nM 5.60
CHEMBL415568 — IC50 = 3981.07 nM 5.40
CHEMBL231056 — IC50 = 3981.07 nM 5.40
CHEMBL415568 — IC50 = 4200.0 nM 5.38
CHEMBL231056 — IC50 = 4400.0 nM 5.36
CHEMBL388212 — IC50 = 11000.0 nM 4.96
CHEMBL388212 — IC50 = 12589.25 nM 4.90
CHEMBL395727 — IC50 = 30000.0 nM 4.52
CHEMBL229999 — IC50 = 30000.0 nM 4.52
CHEMBL415569 — IC50 = 30000.0 nM 4.52
CHEMBL388049 — IC50 = 30000.0 nM 4.52
CHEMBL244561 — IC50 = 30000.0 nM 4.52
CHEMBL415570 — IC50 = 30000.0 nM 4.52
CHEMBL388046 — IC50 = 30000.0 nM 4.52
CHEMBL389120 — IC50 = 30000.0 nM 4.52
CHEMBL395727 — IC50 = 31622.78 nM 4.50
CHEMBL229999 — IC50 = 31622.78 nM 4.50
CHEMBL244561 — IC50 = 31622.78 nM 4.50
CHEMBL415570 — IC50 = 31622.78 nM 4.50
CHEMBL415569 — IC50 = 31622.78 nM 4.50
CHEMBL389120 — IC50 = 31622.78 nM 4.50
CHEMBL388046 — IC50 = 31622.78 nM 4.50
CHEMBL388049 — IC50 = 31622.78 nM 4.50
CHEMBL230952 — IC50 = 100000.0 nM 4.00
CHEMBL230952 — IC50 = 100000.0 nM 4.00
CHEMBL390135 — IC50 = 100000.0 nM 4.00
CHEMBL396705 — IC50 = 100000.0 nM 4.00
CHEMBL396705 — IC50 = 100000.0 nM 4.00
CHEMBL390135 — IC50 = 100000.0 nM 4.00
CHEMBL1180293 — IC50 > 100000.0 nM -
CHEMBL1180293 — IC50 > 100000.0 nM -
CHEMBL231047 TOXIFERINE IC50 > 100000.0 nM -
CHEMBL231047 TOXIFERINE IC50 > 100000.0 nM -
CHEMBL206666 — IC50 > 100000.0 nM -
CHEMBL206666 — IC50 > 100000.0 nM -
CHEMBL382243 — IC50 > 100000.0 nM -
CHEMBL382243 — IC50 > 100000.0 nM -
CHEMBL229998 — IC50 > 100000.0 nM -
CHEMBL229998 — IC50 > 100000.0 nM -
CHEMBL395960 — IC50 > 100000.0 nM -
CHEMBL395960 — IC50 > 100000.0 nM -
CHEMBL510275 METHYLLYCACONITINE IC50 - — -
CHEMBL96 GAMMA-AMINOBUTYRIC ACID EC50 - — -
CHEMBL667 ACETYLCHOLINE EC50 - — -
CHEMBL773 GLYCINE EC50 - — -