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Assay Detail

CHEMBL896287

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Functional
Antagonist activity at rat alpha3beta4 nAChR 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 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907593) ↗
Type PROTEIN COMPLEX
Organism Rattus norvegicus

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 4.49 5.00
EC50 5 5.08 5.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL667 ACETYLCHOLINE 4.0 2 5.10
CHEMBL388212 — — 2 5.00
CHEMBL1180293 — — 2 4.80
CHEMBL388048 — — 2 4.80
CHEMBL395727 — — 2 4.52
CHEMBL231047 TOXIFERINE — 2 4.52
CHEMBL415569 — — 2 4.52
CHEMBL415568 — — 2 4.52
CHEMBL244561 — — 2 4.52
CHEMBL231056 — — 2 4.52
CHEMBL388049 — — 2 4.50
CHEMBL390135 — — 2 4.00
CHEMBL230952 — — 2 4.00
CHEMBL229999 — — 2 -
CHEMBL206666 — — 2 -
CHEMBL382243 — — 2 -
CHEMBL415570 — — 2 -
CHEMBL229998 — — 2 -
CHEMBL388046 — — 2 -
CHEMBL389120 — — 2 -
CHEMBL396705 — — 2 -
CHEMBL96 GAMMA-AMINOBUTYRIC ACID 1.0 1 -
CHEMBL395960 — — 2 -
CHEMBL510275 METHYLLYCACONITINE — 1 -
CHEMBL773 GLYCINE 4.0 1 -
CHEMBL39 SEROTONIN 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL667 ACETYLCHOLINE EC50 = 7943.28 nM 5.10
CHEMBL667 ACETYLCHOLINE EC50 = 8700.0 nM 5.06
CHEMBL388212 — IC50 = 10000.0 nM 5.00
CHEMBL388212 — IC50 = 11000.0 nM 4.96
CHEMBL388048 — IC50 = 15848.93 nM 4.80
CHEMBL388048 — IC50 = 16000.0 nM 4.80
CHEMBL1180293 — IC50 = 15848.93 nM 4.80
CHEMBL1180293 — IC50 = 18000.0 nM 4.75
CHEMBL244561 — IC50 = 30000.0 nM 4.52
CHEMBL395727 — IC50 = 30000.0 nM 4.52
CHEMBL415569 — IC50 = 30000.0 nM 4.52
CHEMBL415568 — IC50 = 30000.0 nM 4.52
CHEMBL231056 — IC50 = 30000.0 nM 4.52
CHEMBL231047 TOXIFERINE IC50 = 30000.0 nM 4.52
CHEMBL244561 — IC50 = 31622.78 nM 4.50
CHEMBL231056 — IC50 = 31622.78 nM 4.50
CHEMBL231047 TOXIFERINE IC50 = 31622.78 nM 4.50
CHEMBL415568 — IC50 = 31622.78 nM 4.50
CHEMBL415569 — IC50 = 31622.78 nM 4.50
CHEMBL388049 — IC50 = 31622.78 nM 4.50
CHEMBL395727 — 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
CHEMBL388049 — IC50 = 100000.0 nM 4.00
CHEMBL390135 — IC50 = 100000.0 nM 4.00
CHEMBL229999 — IC50 > 100000.0 nM -
CHEMBL229999 — IC50 > 100000.0 nM -
CHEMBL206666 — IC50 > 100000.0 nM -
CHEMBL206666 — IC50 > 100000.0 nM -
CHEMBL382243 — IC50 > 100000.0 nM -
CHEMBL382243 — IC50 > 100000.0 nM -
CHEMBL415570 — IC50 > 100000.0 nM -
CHEMBL415570 — IC50 > 100000.0 nM -
CHEMBL510275 METHYLLYCACONITINE IC50 - — -
CHEMBL229998 — IC50 > 100000.0 nM -
CHEMBL229998 — IC50 > 100000.0 nM -
CHEMBL388046 — IC50 > 100000.0 nM -
CHEMBL388046 — IC50 > 100000.0 nM -
CHEMBL389120 — IC50 > 100000.0 nM -
CHEMBL389120 — IC50 > 100000.0 nM -
CHEMBL396705 — IC50 > 100000.0 nM -
CHEMBL396705 — IC50 > 100000.0 nM -
CHEMBL96 GAMMA-AMINOBUTYRIC ACID EC50 - — -
CHEMBL395960 — IC50 > 100000.0 nM -
CHEMBL395960 — IC50 > 100000.0 nM -
CHEMBL773 GLYCINE EC50 - — -
CHEMBL39 SEROTONIN EC50 - — -