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Compound Detail

CHEMBL1719232

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CC(C)Oc1cccc(-c2cnc(N3CCC(C(N)=O)CC3)s2)c1

Basic Information

ChEMBL ID CHEMBL1719232
Phase Preclinical
Structure Type MOL
InChI Key IMZSWXAOQBTCCW-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
11
PK Parameters
7
Publications
0
Known Names

Molecular Properties

345.5
MW (Da)
3.30
ALogP
5
HBA
1
HBD
68.5
PSA (Ų)
0.90
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H23N3O2S
MW 345.47
Aromatic Rings 2
Heavy Atoms 24
NP-Likeness -1.72

Activity Summary

IC50 1 meas. best 6.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Luciferin 4-monooxygenase
CHEMBL3701
IC50 6.1 6.1 800.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1857.0 ng.hr.mL-1 Mus musculus
AUC 1429.0 ng.hr.mL-1 Mus musculus
AUC 546.0 ng.hr.mL-1 Mus musculus
AUC 607.0 ng.hr.mL-1 Mus musculus
Cmax 3720.0 nM Mus musculus
Cmax 1.28 umol/Kg Mus musculus
T1/2 0.5 hr Mus musculus
T1/2 5.78 hr Mus musculus
T1/2 5.44 hr Mus musculus
Tmax 0.083 hr Mus musculus
Tmax 0.083 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Luciferin 4-monooxygenase IC50 = 800.0 nM 6.1 Inhibition of fire fly luciferase 21819082

Literature References

PubMed DOI Target Context # Activities
21819082 10.1021/jm200497t Plasma 14
21819082 10.1021/jm200497t Brain 14
21819082 10.1021/jm200497t Survival motor neuron protein 2
21819082 10.1021/jm200497t Caco-2 2
21819082 10.1021/jm200497t Luciferin 4-monooxygenase 1
21819082 10.1021/jm200497t Liver 1
21819082 10.1021/jm200497t ADMET 1

Data from ChEMBL 36 via Core Engine