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Compound Detail

CHEMBL222946

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CCN(CCCCCC(=O)N1CCC(CC2CCN(C(=O)CCCCCN(CC)Cc3ccccc3OC)CC2)CC1)Cc1ccccc1OC.O=C(O)C(=O)O

Basic Information

ChEMBL ID CHEMBL222946
Phase Preclinical
Structure Type MOL
InChI Key KHJKFCLBRSESSE-UHFFFAOYSA-N
Parent Compound CHEMBL1182221
Active Moiety CHEMBL1182221
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

705.0
MW (Da)
8.04
ALogP
6
HBA
0
HBD
65.6
PSA (Ų)
0.12
QED
2
Ro5 Violations
22
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C45H70N4O8
MW 795.07
Aromatic Rings 2
Heavy Atoms 51
NP-Likeness -0.56

Activity Summary

IC50 2 meas. best 8.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 8.48 8.48 3.3 1
Cholinesterase
CHEMBL1914
IC50 5.19 5.19 6456.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 3.311 nM 8.48 Inhibition of human recombinant AChE 15588084
Cholinesterase IC50 = 6456.54 nM 5.19 Inhibition of human recombinant BChE 15588084

Literature References

PubMed DOI Target Context # Activities
15588084 10.1021/jm0494366 Acetylcholinesterase 2
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