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Compound Detail

CHEMBL3289718

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COC(=O)[C@@]1(C)CC[C@]2(C)CC[C@]3(C)C(=CC(=O)[C@@H]4[C@@]5(C)CC[C@H](OC(=O)[C@@H](N)CCC(=O)OCc6ccccc6)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]2C1

Basic Information

ChEMBL ID CHEMBL3289718
Phase Preclinical
Structure Type MOL
InChI Key FHLUPNCWSRMRAC-FHNBYQFJSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

704.0
MW (Da)
7.90
ALogP
8
HBA
1
HBD
122.0
PSA (Ų)
0.21
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C43H61NO7
MW 703.96
Aromatic Rings 1
Heavy Atoms 51
NP-Likeness 2.21

Activity Summary

Ki 1 meas. best 4.79

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL4078
Ki 4.79 4.79 16050.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase Ki = 16050.0 nM 4.79 Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as su... 24853320

Literature References

PubMed DOI Target Context # Activities
24853320 10.1016/j.bmc.2014.04.046 Acetylcholinesterase 2
24853320 10.1016/j.bmc.2014.04.046 Cholinesterase 2
24853320 10.1016/j.bmc.2014.04.046 Unchecked 2
24853320 10.1016/j.bmc.2014.04.046 Papain 1
24853320 10.1016/j.bmc.2014.04.046 Carbonic anhydrase 2 1
24853320 10.1016/j.bmc.2014.04.046 ADMET 1

Data from ChEMBL 36 via Core Engine