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Compound Detail

CHEMBL107077

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COc1ccc(Sc2ccccc2CN(C)C)c(N)c1

Basic Information

ChEMBL ID CHEMBL107077
Phase Preclinical
Structure Type MOL
InChI Key HYOCZQPMJUZYKD-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
1
PK Parameters
7
Publications
0
Known Names

Molecular Properties

288.4
MW (Da)
3.49
ALogP
4
HBA
1
HBD
38.5
PSA (Ų)
0.85
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H20N2OS
MW 288.42
Aromatic Rings 2
Heavy Atoms 20
NP-Likeness -0.88

Activity Summary

Ki 4 meas. best 8.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent serotonin transporter
CHEMBL313
Ki 8.96 8.96 1.1 1
Sodium-dependent serotonin transporter
CHEMBL228
Ki 8.72 8.72 1.9 1
Sodium-dependent noradrenaline transporter
CHEMBL222
Ki 5.7 5.7 1992.0 1
Sodium-dependent dopamine transporter
CHEMBL238
Ki 5.58 5.58 2651.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.3133 hr -

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10956218 10.1021/jm000079i Rattus norvegicus 35
10956218 10.1021/jm000079i Sodium-dependent serotonin transporter 1
10956218 10.1021/jm000079i Sodium-dependent noradrenaline transporter 1
10956218 10.1021/jm000079i Sodium-dependent dopamine transporter 1
10956218 10.1021/jm000079i ADMET 1
10956218 10.1021/jm000079i No relevant target 1
12361398 10.1021/jm020167y Sodium-dependent serotonin transporter 1

Data from ChEMBL 36 via Core Engine