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Compound Detail

CHEMBL4078221

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CC(=O)O[C@H]1CC[C@]2(C)[C@H]3CC[C@@H]4[C@H]5[C@H](/C(C)=N/O)CC[C@]5(C(=O)O)CC[C@@]4(C)[C@]3(C)CC[C@H]2C1(C)C

Basic Information

ChEMBL ID CHEMBL4078221
Phase Preclinical
Structure Type MOL
InChI Key YJOCZVZYORIYKP-XINVUCMASA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

515.7
MW (Da)
6.93
ALogP
5
HBA
2
HBD
96.2
PSA (Ų)
0.18
QED
2
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H49NO5
MW 515.74
Aromatic Rings 0
Heavy Atoms 37
NP-Likeness 2.64

Activity Summary

Ki 1 meas. best 4.78

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL4078
Ki 4.78 4.78 16710.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase Ki = 16710.0 nM 4.78 Competitive inhibition of electric eel AChE using acetylthiocholine iodide as su... 27936444

Literature References

PubMed DOI Target Context # Activities
27936444 10.1016/j.ejmech.2016.11.056 Cholinesterase 2
27936444 10.1016/j.ejmech.2016.11.056 No relevant target 2
27936444 10.1016/j.ejmech.2016.11.056 Acetylcholinesterase 1
27936444 10.1016/j.ejmech.2016.11.056 Unchecked 1

Data from ChEMBL 36 via Core Engine