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Compound Detail

CHEMBL2206429

DIMETHYLAMINOMICHELIOLIDE HYDROCHLORIDE
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CC1=C2CC[C@@](C)(O)[C@@H]2[C@H]2OC(=O)[C@@H](CN(C)C)[C@@H]2CC1.Cl

Basic Information

ChEMBL ID CHEMBL2206429
Name DIMETHYLAMINOMICHELIOLIDE HYDROCHLORIDE
Phase Preclinical
Structure Type MOL
InChI Key ZKHJWBSQJWCFMA-GMFVQMBMSA-N
Parent Compound CHEMBL2220079
Active Moiety CHEMBL2220079
2
Targets
2
Activities
1
Assay Types
18
PK Parameters
5
Publications
0
Known Names

Molecular Properties

293.4
MW (Da)
1.98
ALogP
4
HBA
1
HBD
49.8
PSA (Ų)
0.62
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H28ClNO3
MW 329.87
Aromatic Rings 0
Heavy Atoms 21
NP-Likeness 2.36

Activity Summary

IC50 2 meas. best 4.76

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HL-60
CHEMBL383
IC50 4.76 4.76 17200.0 1
NON-PROTEIN TARGET
CHEMBL3879801
IC50 4.67 4.67 21500.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 44812.3 ng.hr.mL-1 Mus musculus
AUC 43943.7 ng.hr.mL-1 Mus musculus
AUC 50326.8 ng.hr.mL-1 Mus musculus
AUC 49633.6 ng.hr.mL-1 Mus musculus
CL 37.67 mL.min-1.kg-1 Mus musculus
CL 51.33 mL.min-1.kg-1 Mus musculus
Cmax 316621.79 nM Mus musculus
Cmax 64653.56 nM Mus musculus
F 75.0 % Mus musculus
MRT 3.52 hr Mus musculus
MRT 1.51 hr Mus musculus
MRT 9.85 hr Mus musculus
MRT 8.85 hr Mus musculus
T1/2 18.92 hr Mus musculus
T1/2 9.82 hr Mus musculus
Tmax 0.19 hr Mus musculus
Vd 88.18 L.kg-1 Mus musculus
Vd 47.38 L.kg-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22985027 10.1021/jm301064b Mus musculus 30
22985027 10.1021/jm301064b NON-PROTEIN TARGET 10
22985027 10.1021/jm301064b No relevant target 3
22985027 10.1021/jm301064b Plasma 1
22985027 10.1021/jm301064b HL-60 1

Data from ChEMBL 36 via Core Engine