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Assay Detail

CHEMBL896285

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Binding
Displacement of [3H]GR65630 from human 5HT3A receptor in HEK293 cells
ChEMBL ↗
49
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 49 4.98 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18772 QUIPAZINE 2.0 2 8.43
CHEMBL388048 — — 2 5.72
CHEMBL231056 — — 2 5.60
CHEMBL388212 — — 2 5.51
CHEMBL388046 — — 2 5.24
CHEMBL415568 — — 2 5.23
CHEMBL395727 — — 2 5.00
CHEMBL230952 — — 2 4.82
CHEMBL244561 — — 2 4.72
CHEMBL229998 — — 2 4.64
CHEMBL389120 — — 2 4.60
CHEMBL415569 — — 2 4.40
CHEMBL388049 — — 2 4.00
CHEMBL390135 — — 2 4.00
CHEMBL396705 — — 2 4.00
CHEMBL415570 — — 2 4.00
CHEMBL3 NICOTINE 4.0 1 -
CHEMBL1180293 — — 2 -
CHEMBL388047 — — 1 -
CHEMBL231047 TOXIFERINE — 2 -
CHEMBL203627 — — 2 -
CHEMBL510275 METHYLLYCACONITINE — 1 -
CHEMBL395960 — — 2 -
CHEMBL382243 — — 2 -
CHEMBL206666 — — 2 -
CHEMBL229999 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18772 QUIPAZINE Ki = 3.7 nM 8.43
CHEMBL18772 QUIPAZINE Ki = 3.981 nM 8.40
CHEMBL388048 — Ki = 1900.0 nM 5.72
CHEMBL388048 — Ki = 1995.26 nM 5.70
CHEMBL231056 — Ki = 2511.89 nM 5.60
CHEMBL231056 — Ki = 2700.0 nM 5.57
CHEMBL388212 — Ki = 3100.0 nM 5.51
CHEMBL388212 — Ki = 3162.28 nM 5.50
CHEMBL388046 — Ki = 5700.0 nM 5.24
CHEMBL415568 — Ki = 5900.0 nM 5.23
CHEMBL388046 — Ki = 6309.57 nM 5.20
CHEMBL415568 — Ki = 6309.57 nM 5.20
CHEMBL395727 — Ki = 10000.0 nM 5.00
CHEMBL395727 — Ki = 11000.0 nM 4.96
CHEMBL230952 — Ki = 15000.0 nM 4.82
CHEMBL230952 — Ki = 15848.93 nM 4.80
CHEMBL244561 — Ki = 19000.0 nM 4.72
CHEMBL244561 — Ki = 19952.62 nM 4.70
CHEMBL229998 — Ki = 23000.0 nM 4.64
CHEMBL389120 — Ki = 25118.86 nM 4.60
CHEMBL229998 — Ki = 25118.86 nM 4.60
CHEMBL389120 — Ki = 28000.0 nM 4.55
CHEMBL415569 — Ki = 40000.0 nM 4.40
CHEMBL415569 — Ki = 39810.72 nM 4.40
CHEMBL388049 — Ki = 100000.0 nM 4.00
CHEMBL388049 — Ki = 100000.0 nM 4.00
CHEMBL415570 — Ki = 100000.0 nM 4.00
CHEMBL415570 — Ki = 100000.0 nM 4.00
CHEMBL396705 — Ki = 100000.0 nM 4.00
CHEMBL390135 — Ki = 100000.0 nM 4.00
CHEMBL390135 — Ki = 100000.0 nM 4.00
CHEMBL396705 — Ki = 100000.0 nM 4.00
CHEMBL388047 — Ki - — -
CHEMBL203627 — Ki > 100000.0 nM -
CHEMBL382243 — Ki > 100000.0 nM -
CHEMBL1180293 — Ki > 100000.0 nM -
CHEMBL1180293 — Ki > 100000.0 nM -
CHEMBL3 NICOTINE Ki - — -
CHEMBL203627 — Ki > 100000.0 nM -
CHEMBL510275 METHYLLYCACONITINE Ki - — -
CHEMBL231047 TOXIFERINE Ki > 100000.0 nM -
CHEMBL395960 — Ki > 100000.0 nM -
CHEMBL382243 — Ki > 100000.0 nM -
CHEMBL206666 — Ki > 100000.0 nM -
CHEMBL206666 — Ki > 100000.0 nM -
CHEMBL229999 — Ki > 100000.0 nM -
CHEMBL229999 — Ki > 100000.0 nM -
CHEMBL231047 TOXIFERINE Ki > 100000.0 nM -
CHEMBL395960 — Ki > 100000.0 nM -