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Compound Detail

CHEMBL1224265

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NC(=O)n1ccc(-c2ccc(-c3ccccc3Cl)cc2)n1

Basic Information

ChEMBL ID CHEMBL1224265
Phase Preclinical
Structure Type MOL
InChI Key ATSGXTVRKKTJHN-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

297.8
MW (Da)
3.80
ALogP
3
HBA
1
HBD
60.9
PSA (Ų)
0.78
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H12ClN3O
MW 297.75
Aromatic Rings 3
Heavy Atoms 21
NP-Likeness -1.14

Activity Summary

Ki 1 meas. best 9.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium channel protein type 9 subunit alpha
CHEMBL4296
Ki 9.96 9.96 0.1 1

Pharmacokinetic Data

Parameter Value Units Species
CL 125.0 mL.min-1.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sodium channel protein type 9 subunit alpha Ki = 0.111 nM 9.96 Inhibition of human Nav 1.7 channel by electrophysiology 20709545

Literature References

PubMed DOI Target Context # Activities
20709545 10.1016/j.bmcl.2010.07.080 Sodium channel protein type 9 subunit alpha 1
20709545 10.1016/j.bmcl.2010.07.080 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine