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Compound Detail

CHEMBL521463

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Cn1cc(S(=O)(=O)N2CCC(CNC(=O)c3ccc(Cl)cc3Cl)(c3ncccc3F)CC2)nn1

Basic Information

ChEMBL ID CHEMBL521463
Phase Preclinical
Structure Type MOL
InChI Key WFJSYNMBPNICIS-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
6
Publications
0
Known Names

Molecular Properties

527.4
MW (Da)
2.81
ALogP
7
HBA
1
HBD
110.1
PSA (Ų)
0.53
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H21Cl2FN6O3S
MW 527.41
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.82

Activity Summary

IC50 1 meas. best 9.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium- and chloride-dependent glycine transporter 1
CHEMBL2337
IC50 9.19 9.19 0.7 1

Pharmacokinetic Data

Parameter Value Units Species
F 3.0 % Rattus norvegicus
T1/2 0.3 hr 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 Liver microsomes 2
19318248 10.1016/j.bmcl.2009.02.102 Rattus norvegicus 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