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Compound Detail

CHEMBL3216788

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Cl.Cl.c1ccc2c3c([nH]c2c1)[C@H]1[C@H]2CC[C@H]([C@@H]4CCCN[C@@H]42)N1CC3

Basic Information

ChEMBL ID CHEMBL3216788
Phase Preclinical
Structure Type MOL
InChI Key AJFJKGLXKPEJMU-WJSUCZTPSA-N
Parent Compound CHEMBL2219846
Active Moiety CHEMBL2219846
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

307.4
MW (Da)
3.23
ALogP
2
HBA
2
HBD
31.1
PSA (Ų)
0.78
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H27Cl2N3
MW 380.36
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness 0.81

Activity Summary

IC50 2 meas. best 5.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL1914
IC50 5.04 5.04 9010.0 1
Cholinesterase
CHEMBL5763
IC50 4.97 4.97 10630.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cholinesterase IC50 = 9010.0 nM 5.04 Inhibition of human BChE by Ellman's method 23062825
Cholinesterase IC50 = 10630.0 nM 4.97 Inhibition of horse 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

Data from ChEMBL 36 via Core Engine