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Compound Detail

CHEMBL3621334

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CC[N+]1(Cc2ccccc2[N+](=O)[O-])CCCCCn2c(C)cc(=O)n(c2=O)CCCCC[N+](CC)(Cc2ccccc2[N+](=O)[O-])CCCCCn2c(=O)cc(C)n(c2=O)CCCCC1.[Br-].[Br-]

Basic Information

ChEMBL ID CHEMBL3621334
Phase Preclinical
Structure Type MOL
InChI Key GGWDQIWDSOCPKA-UHFFFAOYSA-L
Parent Compound CHEMBL3623941
Active Moiety CHEMBL3623941
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

887.1
MW (Da)
7.24
ALogP
12
HBA
0
HBD
174.3
PSA (Ų)
0.10
QED
3
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C48H70Br2N8O8
MW 1046.94
Aromatic Rings 4
Heavy Atoms 64
NP-Likeness -0.40

Activity Summary

IC50 2 meas. best 6.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 6.89 6.89 130.0 1
Cholinesterase
CHEMBL1914
IC50 5.0 5.0 10000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 130.0 nM 6.89 Inhibition of AChE from human erythrocytes -
Cholinesterase IC50 = 10000.0 nM 5.0 Inhibition of BChE from human plasma -

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C4MD00225C Cholinesterase 1
- 10.1039/C4MD00225C Acetylcholinesterase 1
- 10.1039/C4MD00225C Cholinesterases; ACHE & BCHE 1

Data from ChEMBL 36 via Core Engine