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Assay Detail

CHEMBL816912

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

Binding
Displacement of [3H]vesamicol from Vesamicol receptor of Torpedo californica
14
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Torpedo californica
Confidence 9 — Direct single protein target
Curated By Expert

Target

Vesicular acetylcholine transporter (CHEMBL3313)
Type SINGLE PROTEIN
Organism Torpedo californica

Publication

Acyclic analogues of 2-(4-phenylpiperidino)cyclohexanol (vesamicol): conformationally mobile inhibitors of vesicular acetylcholine transport.
Efange SM, Michelson RH, Dutta AK, Parsons SM.
J Med Chem (1991) 34 : 2638 -2643
PubMed 1875353 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.74 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL89812 4 7.52
CHEMBL20943 1 7.47
CHEMBL314574 1 7.14
CHEMBL84797 1 7.14
CHEMBL90556 1 6.94
CHEMBL88534 1 6.84
CHEMBL89896 1 6.66
CHEMBL88522 1 6.28
CHEMBL89577 1 6.00
CHEMBL314881 1 5.85
CHEMBL87177 1 5.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL89812 IC50 = 30.0 nM 7.52
CHEMBL20943 IC50 = 34.0 nM 7.47
CHEMBL89812 IC50 = 36.0 nM 7.44
CHEMBL314574 IC50 = 73.0 nM 7.14
CHEMBL84797 IC50 = 73.0 nM 7.14
CHEMBL90556 IC50 = 115.0 nM 6.94
CHEMBL88534 IC50 = 145.0 nM 6.84
CHEMBL89812 IC50 = 170.0 nM 6.77
CHEMBL89896 IC50 = 220.0 nM 6.66
CHEMBL89812 IC50 = 328.0 nM 6.48
CHEMBL88522 IC50 = 520.0 nM 6.28
CHEMBL89577 IC50 = 990.0 nM 6.00
CHEMBL314881 IC50 = 1400.0 nM 5.85
CHEMBL87177 IC50 = 1540.0 nM 5.81