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Compound Detail

CHEMBL4522646

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CCc1cc(-c2cnn(C)c2)cc(S(=O)(=O)c2cnc(CN)s2)c1.Cl

Basic Information

ChEMBL ID CHEMBL4522646
Phase Preclinical
Structure Type MOL
InChI Key XAJYHKZTSFGXNC-UHFFFAOYSA-N
Parent Compound CHEMBL4444163
Active Moiety CHEMBL4444163
2
Targets
2
Activities
1
Assay Types
8
PK Parameters
0
Publications
0
Known Names

Molecular Properties

362.5
MW (Da)
2.40
ALogP
7
HBA
1
HBD
90.9
PSA (Ų)
0.75
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H19ClN4O2S2
MW 398.94
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.79

Activity Summary

IC50 2 meas. best 6.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Lysyl oxidase homolog 2
CHEMBL3714029
IC50 6.89 6.89 130.0 1
Unchecked
CHEMBL612545
IC50 6.72 6.72 190.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 6524.64 ng.hr.mL-1 Mus musculus
AUC 6887.12 ng.hr.mL-1 Rattus norvegicus
Cmax 27000.0 nM Mus musculus
Cmax 6500.0 nM Rattus norvegicus
F 48.0 % Mus musculus
F 68.0 % Rattus norvegicus
T1/2 1.1 hr Mus musculus
T1/2 1.3 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Data from ChEMBL 36 via Core Engine