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Compound Detail

CHEMBL4161447

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CC(=N)NCc1cccc(CNC(=O)[C@@H]2CCCN2)c1.Cl.Cl

Basic Information

ChEMBL ID CHEMBL4161447
Phase Preclinical
Structure Type MOL
InChI Key VFWZUEHZTBFYTG-UTLKBRERSA-N
Parent Compound CHEMBL4302051
Active Moiety CHEMBL4302051
1
Targets
2
Activities
1
Assay Types
4
PK Parameters
7
Publications
0
Known Names

Molecular Properties

274.4
MW (Da)
1.14
ALogP
3
HBA
4
HBD
77.0
PSA (Ų)
0.48
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 C15H24Cl2N4O
MW 347.29
Aromatic Rings 1
Heavy Atoms 20
NP-Likeness -0.15

Activity Summary

IC50 2 meas. best 7.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nitric oxide synthase, inducible
CHEMBL3464
IC50 7.24 7.24 58.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 24.0 hr -
T1/2 24.0 hr -
T1/2 24.0 hr -
T1/2 11.0 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29689474 10.1016/j.ejmech.2018.04.027 C6 16
29689474 10.1016/j.ejmech.2018.04.027 Unchecked 5
29689474 10.1016/j.ejmech.2018.04.027 No relevant target 3
29689474 10.1016/j.ejmech.2018.04.027 Nitric oxide synthase, inducible 2
29689474 10.1016/j.ejmech.2018.04.027 Nitric oxide synthase 1 1
29689474 10.1016/j.ejmech.2018.04.027 ADMET 1
29689474 10.1016/j.ejmech.2018.04.027 Nitric oxide synthase 3 1

Data from ChEMBL 36 via Core Engine