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Compound Detail

CHEMBL3288094

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C=C(C=O)[C@@H]1CC[C@]2(C)C(=O)C[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CCC(=O)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]12

Basic Information

ChEMBL ID CHEMBL3288094
Phase Preclinical
Structure Type MOL
InChI Key PEXSLIJXRWANOX-BIPUANEUSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

452.7
MW (Da)
6.59
ALogP
3
HBA
0
HBD
51.2
PSA (Ų)
0.35
QED
1
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H44O3
MW 452.68
Aromatic Rings 0
Heavy Atoms 33
NP-Likeness 2.84

Activity Summary

IC50 1 meas. best 4.67

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL5763
IC50 4.67 4.67 21500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cholinesterase IC50 = 21500.0 nM 4.67 Inhibition of BChE in horse serum using butyrylthiocholine iodide as substrate a... 24835788

Literature References

PubMed DOI Target Context # Activities
24835788 10.1016/j.bmc.2014.04.050 Acetylcholinesterase 2
24835788 10.1016/j.bmc.2014.04.050 Cholinesterase 2
24835788 10.1016/j.bmc.2014.04.050 Unchecked 1

Data from ChEMBL 36 via Core Engine