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Compound Detail

CHEMBL3400467

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CN(c1ccc(Cl)cc1)c1nc(=O)c2cccnc2s1

Basic Information

ChEMBL ID CHEMBL3400467
Phase Preclinical
Structure Type MOL
InChI Key RCGOQPBYNHJZCU-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
8
PK Parameters
3
Publications
0
Known Names

Molecular Properties

303.8
MW (Da)
3.47
ALogP
5
HBA
0
HBD
46.1
PSA (Ų)
0.73
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 C14H10ClN3OS
MW 303.77
Aromatic Rings 3
Heavy Atoms 20
NP-Likeness -1.68

Activity Summary

IC50 1 meas. best 5.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuron
CHEMBL613705
IC50 5.7 5.7 2000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 472.3 ng.hr.mL-1 Rattus norvegicus
AUC 542.0 ng.hr.mL-1 Rattus norvegicus
CL 30.75 mL.min-1.kg-1 Rattus norvegicus
Cmax 1399.41 nM Rattus norvegicus
F 87.1 % Rattus norvegicus
T1/2 0.58 hr Rattus norvegicus
T1/2 0.44 hr Rattus norvegicus
Tmax 0.25 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neuron IC50 = 2000.0 nM 5.7 Inhibition of kainate-induced neurotoxicity in primary rat hippocampal neurons a... 25792143

Literature References

PubMed DOI Target Context # Activities
25792143 10.1016/j.bmc.2015.02.033 Rattus norvegicus 9
25792143 10.1016/j.bmc.2015.02.033 Mus musculus 1
25792143 10.1016/j.bmc.2015.02.033 Neuron 1

Data from ChEMBL 36 via Core Engine