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Compound Detail

CHEMBL222856

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COc1ccccc1CN(C)CCCCCC(=O)N(C)CCCCCCCCN(C)C(=O)CCCCCN(C)Cc1ccccc1OC.O=C(O)C(=O)O

Basic Information

ChEMBL ID CHEMBL222856
Phase Preclinical
Structure Type MOL
InChI Key VBMPKVGQNHLYJG-UHFFFAOYSA-N
Parent Compound CHEMBL11805
Active Moiety CHEMBL11805
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

667.0
MW (Da)
7.65
ALogP
6
HBA
0
HBD
65.6
PSA (Ų)
0.09
QED
2
Ro5 Violations
27
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C42H68N4O8
MW 757.03
Aromatic Rings 2
Heavy Atoms 48
NP-Likeness -0.51

Activity Summary

IC50 2 meas. best 6.77
Ki 1 meas. best 6.98

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
Ki 6.98 6.98 104.0 1
Acetylcholinesterase
CHEMBL220
IC50 6.77 6.77 169.8 1
Cholinesterase
CHEMBL1914
IC50 4.93 4.93 11749.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase Ki = 104.0 nM 6.98 Inhibition of human recombinant AChE 15588084
Acetylcholinesterase IC50 = 169.82 nM 6.77 Inhibition of human recombinant AChE 15588084
Cholinesterase IC50 = 11748.98 nM 4.93 Inhibition of human recombinant BChE 15588084

Literature References

PubMed DOI Target Context # Activities
15588084 10.1021/jm0494366 Acetylcholinesterase 3
15588084 10.1021/jm0494366 Cholinesterase 1
15588084 10.1021/jm0494366 Cholinesterases; ACHE & BCHE 1
15588084 10.1021/jm0494366 Muscarinic acetylcholine receptor M2 1

Data from ChEMBL 36 via Core Engine