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Assay Detail

CHEMBL861245

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

Binding
Displacement of (+/-)-[3H]epibatidine from muscle type nAChR of Torpedo californica in hepes buffer
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Torpedo californica
Tissue Muscle tissue
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Acetylcholine receptor (CHEMBL2096975)
Type PROTEIN COMPLEX
Organism Torpedo californica

Publication

6H,13H-Pyrazino[1,2-a;4,5-a']diindole analogs: probing the pharmacophore for allosteric ligands of muscarinic M2 receptors.
Zlotos DP, Tränkle C, Abdelrahman A, Gündisch D, Radacki K, Braunschweig H, Mohr K.
Bioorg Med Chem Lett (2006) 16 : 1481 -1485
PubMed 16387499 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.76 6.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL382243 1 6.48
CHEMBL206666 1 6.26
CHEMBL607178 DIALLYLCARACURIE V 1 5.82
CHEMBL607179 DIMETHYLCARACURIE V 1 5.28
CHEMBL203627 1 4.97
CHEMBL380352 CARACURINE V 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL382243 Ki = 331.13 nM 6.48
CHEMBL206666 Ki = 549.54 nM 6.26
CHEMBL607178 DIALLYLCARACURIE V Ki = 1513.56 nM 5.82
CHEMBL607179 DIMETHYLCARACURIE V Ki = 5248.07 nM 5.28
CHEMBL203627 Ki = 10715.19 nM 4.97
CHEMBL380352 CARACURINE V Ki < 100000.0 nM -