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Assay Detail

CHEMBL896281

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

Binding
Displacement of [3H]epibatidine from recombinant rat alpha-3-beta-4 nAChr in HEK293 cell line
ChEMBL ↗
49
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 7 — Homologous single protein target
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
Ki 49 4.72 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3 NICOTINE 4.0 2 6.70
CHEMBL1180293 — — 2 5.50
CHEMBL231056 — — 2 4.52
CHEMBL388212 — — 2 4.52
CHEMBL395727 — — 2 4.52
CHEMBL231047 TOXIFERINE — 2 4.52
CHEMBL388048 — — 2 4.52
CHEMBL415568 — — 2 4.52
CHEMBL415569 — — 2 4.00
CHEMBL230952 — — 2 4.00
CHEMBL18772 QUIPAZINE 2.0 1 -
CHEMBL510275 METHYLLYCACONITINE — 1 -
CHEMBL244561 — — 2 -
CHEMBL390135 — — 2 -
CHEMBL395960 — — 2 -
CHEMBL229999 — — 2 -
CHEMBL206666 — — 2 -
CHEMBL203627 — — 2 -
CHEMBL415570 — — 2 -
CHEMBL388049 — — 2 -
CHEMBL388047 — — 1 -
CHEMBL229998 — — 2 -
CHEMBL388046 — — 2 -
CHEMBL389120 — — 2 -
CHEMBL396705 — — 2 -
CHEMBL382243 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3 NICOTINE Ki = 199.53 nM 6.70
CHEMBL3 NICOTINE Ki = 220.0 nM 6.66
CHEMBL1180293 — Ki = 3162.28 nM 5.50
CHEMBL1180293 — Ki = 3200.0 nM 5.50
CHEMBL231047 TOXIFERINE Ki = 30000.0 nM 4.52
CHEMBL415568 — Ki = 30000.0 nM 4.52
CHEMBL388048 — Ki = 30000.0 nM 4.52
CHEMBL395727 — Ki = 30000.0 nM 4.52
CHEMBL388212 — Ki = 30000.0 nM 4.52
CHEMBL231056 — Ki = 30000.0 nM 4.52
CHEMBL231056 — Ki = 31622.78 nM 4.50
CHEMBL388048 — Ki = 31622.78 nM 4.50
CHEMBL415568 — Ki = 31622.78 nM 4.50
CHEMBL231047 TOXIFERINE Ki = 31622.78 nM 4.50
CHEMBL395727 — Ki = 31622.78 nM 4.50
CHEMBL388212 — Ki = 31622.78 nM 4.50
CHEMBL230952 — Ki = 100000.0 nM 4.00
CHEMBL415569 — Ki = 100000.0 nM 4.00
CHEMBL230952 — Ki = 100000.0 nM 4.00
CHEMBL415569 — Ki = 100000.0 nM 4.00
CHEMBL395960 — Ki > 100000.0 nM -
CHEMBL390135 — Ki > 100000.0 nM -
CHEMBL390135 — Ki > 100000.0 nM -
CHEMBL229999 — Ki > 100000.0 nM -
CHEMBL229999 — Ki > 100000.0 nM -
CHEMBL206666 — Ki > 100000.0 nM -
CHEMBL206666 — Ki > 100000.0 nM -
CHEMBL382243 — Ki > 100000.0 nM -
CHEMBL382243 — Ki > 100000.0 nM -
CHEMBL203627 — Ki > 100000.0 nM -
CHEMBL203627 — Ki > 100000.0 nM -
CHEMBL415570 — Ki > 100000.0 nM -
CHEMBL415570 — Ki > 100000.0 nM -
CHEMBL388049 — Ki > 100000.0 nM -
CHEMBL395960 — Ki > 100000.0 nM -
CHEMBL18772 QUIPAZINE Ki - — -
CHEMBL510275 METHYLLYCACONITINE Ki - — -
CHEMBL396705 — Ki > 100000.0 nM -
CHEMBL396705 — Ki > 100000.0 nM -
CHEMBL389120 — Ki > 100000.0 nM -
CHEMBL389120 — Ki > 100000.0 nM -
CHEMBL388046 — Ki > 100000.0 nM -
CHEMBL388049 — Ki > 100000.0 nM -
CHEMBL229998 — Ki > 100000.0 nM -
CHEMBL229998 — Ki > 100000.0 nM -
CHEMBL388047 — Ki - — -
CHEMBL244561 — Ki > 100000.0 nM -
CHEMBL244561 — Ki > 100000.0 nM -
CHEMBL388046 — Ki > 100000.0 nM -