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Compound Detail

CHEMBL464724

VERATRAMINE
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Cc1c([C@H](C)[C@@H]2NC[C@@H](C)C[C@H]2O)ccc2c1C[C@H]1[C@H]2CC=C2C[C@@H](O)CC[C@@]21C

Basic Information

ChEMBL ID CHEMBL464724
Name VERATRAMINE
Phase Preclinical
Structure Type MOL
InChI Key MALFODICFSIXPO-KFKQDBFTSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

409.6
MW (Da)
4.59
ALogP
3
HBA
3
HBD
52.5
PSA (Ų)
0.63
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C27H39NO2
MW 409.61
Aromatic Rings 1
Heavy Atoms 30
NP-Likeness 2.54

Activity Summary

IC50 2 meas. best 4.97

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL5763
IC50 4.97 4.97 10780.0 1
Cholinesterase
CHEMBL1914
IC50 4.71 4.71 19460.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cholinesterase IC50 = 10780.0 nM 4.97 Inhibition of horse BChE by Ellman's method 23062825
Cholinesterase IC50 = 19460.0 nM 4.71 Inhibition of human BChE by Ellman's method 23062825

Literature References

PubMed DOI Target Context # Activities
23062825 10.1016/j.bmc.2012.09.040 Cholinesterase 3
23062825 10.1016/j.bmc.2012.09.040 Acetylcholinesterase 2
- 10.1007/s00044-013-0495-6 PC-3 2
9461666 10.1021/np9703611 Vero 1
20708941 10.1016/j.bmc.2010.07.038 Unchecked 1

Data from ChEMBL 36 via Core Engine