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Compound Detail

CHEMBL484179

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Cn1cc(S(=O)(=O)N2CCC(CNC(=O)c3ccc(Cl)cc3Cl)(CC3CC3)CC2)nn1

Basic Information

ChEMBL ID CHEMBL484179
Phase Preclinical
Structure Type MOL
InChI Key HLFJDXYWHBEFOS-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
6
Publications
0
Known Names

Molecular Properties

486.4
MW (Da)
3.12
ALogP
6
HBA
1
HBD
97.2
PSA (Ų)
0.65
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H25Cl2N5O3S
MW 486.43
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -1.59

Activity Summary

IC50 1 meas. best 7.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium- and chloride-dependent glycine transporter 1
CHEMBL2337
IC50 7.5 7.5 32.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 39.0 mL.min-1.kg-1 Rattus norvegicus
F 27.0 % Rattus norvegicus
T1/2 1.1 hr Rattus norvegicus
Vd 2.2 L.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19318248 10.1016/j.bmcl.2009.02.102 Rattus norvegicus 4
19318248 10.1016/j.bmcl.2009.02.102 Liver microsomes 2
19318248 10.1016/j.bmcl.2009.02.102 Sodium- and chloride-dependent glycine transporter 1 1
19318248 10.1016/j.bmcl.2009.02.102 ADMET 1
19318248 10.1016/j.bmcl.2009.02.102 Mus musculus 1
19318248 10.1016/j.bmcl.2009.02.102 Sodium- and chloride-dependent glycine transporter 2 1

Data from ChEMBL 36 via Core Engine