Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3624575

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

Binding
Displacement of [3H]epibatidine from rat neuronal acetylcholine receptor subunit alpha3beta4 expressed in HEK293 cell membranes incubated for 4 hrs by scintillation counting method
ChEMBL ↗
38
Total Activities
19
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

Conformationally restrained carbamoylcholine homologues. Synthesis, pharmacology at neuronal nicotinic acetylcholine receptors and biostructural considerations.
de la Fuente Revenga M, Balle T, Jensen AA, Frølund B.
Eur J Med Chem (2015) 102 : 352 -362
PubMed 26298493 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 38 5.08 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL486572 — — 2 7.70
CHEMBL3 NICOTINE 4.0 2 6.54
CHEMBL3622596 — — 2 5.19
CHEMBL466400 — — 2 5.00
CHEMBL3622594 — — 2 4.87
CHEMBL3622597 — — 2 4.52
CHEMBL3622595 — — 2 4.30
CHEMBL3622600 — — 2 4.30
CHEMBL3622601 — — 2 4.00
CHEMBL3622606 — — 2 -
CHEMBL3622605 — — 2 -
CHEMBL3622604 — — 2 -
CHEMBL3622603 — — 2 -
CHEMBL3622602 — — 2 -
CHEMBL3622599 — — 2 -
CHEMBL3622598 — — 2 -
CHEMBL3622591 — — 2 -
CHEMBL3622592 — — 2 -
CHEMBL3622593 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL486572 — Ki = 19.95 nM 7.70
CHEMBL3 NICOTINE Ki = 290.0 nM 6.54
CHEMBL3 NICOTINE Ki = 288.4 nM 6.54
CHEMBL486572 — Ki = 420.0 nM 6.38
CHEMBL3622596 — Ki = 6400.0 nM 5.19
CHEMBL3622596 — Ki = 6456.54 nM 5.19
CHEMBL466400 — Ki = 10000.0 nM 5.00
CHEMBL466400 — Ki = 10000.0 nM 5.00
CHEMBL3622594 — Ki = 13489.63 nM 4.87
CHEMBL3622594 — Ki = 14000.0 nM 4.85
CHEMBL3622597 — Ki = 30000.0 nM 4.52
CHEMBL3622597 — Ki = 31622.78 nM 4.50
CHEMBL3622600 — Ki = 50000.0 nM 4.30
CHEMBL3622600 — Ki = 50118.72 nM 4.30
CHEMBL3622595 — Ki = 50118.72 nM 4.30
CHEMBL3622595 — Ki = 50000.0 nM 4.30
CHEMBL3622601 — Ki = 100000.0 nM 4.00
CHEMBL3622601 — Ki = 100000.0 nM 4.00
CHEMBL3622593 — Ki > 1000000.0 nM -
CHEMBL3622598 — Ki = 300000.0 nM -
CHEMBL3622599 — Ki > 1000000.0 nM -
CHEMBL3622602 — Ki > 1000000.0 nM -
CHEMBL3622603 — Ki > 1000000.0 nM -
CHEMBL3622604 — Ki > 1000000.0 nM -
CHEMBL3622605 — Ki = 300000.0 nM -
CHEMBL3622606 — Ki = 300000.0 nM -
CHEMBL3622591 — Ki = 300000.0 nM -
CHEMBL3622591 — Ki = 316227.77 nM -
CHEMBL3622592 — Ki = 1000000.0 nM -
CHEMBL3622593 — Ki > 1000000.0 nM -
CHEMBL3622592 — Ki = 1000000.0 nM -
CHEMBL3622605 — Ki = 316227.77 nM -
CHEMBL3622604 — Ki > 1000000.0 nM -
CHEMBL3622603 — Ki > 1000000.0 nM -
CHEMBL3622606 — Ki = 316227.77 nM -
CHEMBL3622599 — Ki > 1000000.0 nM -
CHEMBL3622598 — Ki = 316227.77 nM -
CHEMBL3622602 — Ki > 1000000.0 nM -