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Compound Detail

CHEMBL1672374

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[O-][S+](CCNCCCc1ccccc1)C(c1ccccc1)c1ccccc1

Basic Information

ChEMBL ID CHEMBL1672374
Phase Preclinical
Structure Type MOL
InChI Key QCMUGORVKCWDCX-UHFFFAOYSA-N
4
Targets
12
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

377.6
MW (Da)
4.75
ALogP
2
HBA
1
HBD
35.1
PSA (Ų)
0.41
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H27NOS
MW 377.55
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.15

Activity Summary

Ki 12 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent serotonin transporter
CHEMBL313
Ki 7.0 6.25 100.0 4
Sodium-dependent dopamine transporter
CHEMBL338
Ki 6.71 6.71 194.0 4
Unchecked
CHEMBL612545
Ki 5.63 5.63 2350.0 1
Transporter
CHEMBL6184
Ki 5.63 5.63 2350.0 3

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sodium-dependent serotonin transporter Ki = 100.0 nM 7.0 Displacement of [3H]citalopram from SERT in Sprague-Dawley rat brain membranes 21344069
Sodium-dependent dopamine transporter Ki = 194.0 nM 6.71 Displacement of [3H]WIN35428 from DAT in Sprague-Dawley rat brain membranes 21344069
Sodium-dependent dopamine transporter Ki = 194.0 nM 6.71 Dopamine Transporter Binding Assay: Brains from male Sprague-Dawley rats weighin... -
Sodium-dependent dopamine transporter Ki = 194.0 nM 6.71 Binding Assay: Dopamine Transporter Binding Assay. Brains from male Sprague-Dawl... -
Sodium-dependent dopamine transporter Ki = 194.0 nM 6.71 Dopamine Transporter Binding Assay: Dopamine Transporter Binding Assay. Brains f... -
Sodium-dependent serotonin transporter Ki = 1000.0 nM 6.0 Serotonin Transporter Binding Assay: Brains from male Sprague-Dawley rats weighi... -
Sodium-dependent serotonin transporter Ki = 1000.0 nM 6.0 Binding Assay: Serotonin Transporter Binding Assay. Brains from male Sprague-Daw... -
Sodium-dependent serotonin transporter Ki = 1000.0 nM 6.0 Serotonin Transporter Binding Assay: Serotonin Transporter Binding Assay. Brains... -
Transporter Ki = 2350.0 nM 5.63 Displacement of [3H]nisoxetine from NET in Sprague-Dawley rat brain membranes 21344069
Transporter Ki = 2350.0 nM 5.63 Norepinephrine Transporter Binding Assay: Brains from male Sprague-Dawley rats w... -
Unchecked Ki = 2350.0 nM 5.63 Binding Assay: Norepinephrine Transporter Binding Assay. Brains from male Spragu... -
Transporter Ki = 2350.0 nM 5.63 Norepinephrine Transporter Binding Assay: Norepinephrine Transporter Binding Ass... -

Literature References

PubMed DOI Target Context # Activities
21344069 10.1021/ml1002025 Sodium-dependent dopamine transporter 1
21344069 10.1021/ml1002025 Sodium-dependent serotonin transporter 1
21344069 10.1021/ml1002025 Transporter 1

Data from ChEMBL 36 via Core Engine