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Compound Detail

CHEMBL3323095

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CN1Cc2ccccc2C(c2ccc3sccc3c2)C1

Basic Information

ChEMBL ID CHEMBL3323095
Phase Preclinical
Structure Type MOL
InChI Key MHFUBIDIXOMIAL-UHFFFAOYSA-N
4
Targets
13
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

279.4
MW (Da)
4.48
ALogP
2
HBA
0
HBD
3.2
PSA (Ų)
0.63
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H17NS
MW 279.41
Aromatic Rings 3
Heavy Atoms 20
NP-Likeness -0.73

Activity Summary

IC50 7 meas. best 8.77
Ki 6 meas. best 8.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent noradrenaline transporter
CHEMBL222
Ki 8.92 8.92 1.2 2
Sodium-dependent serotonin transporter
CHEMBL228
IC50 8.77 7.965 1.7 2
Sodium-dependent noradrenaline transporter
CHEMBL222
IC50 8.47 7.465 3.4 2
Sodium-dependent dopamine transporter
CHEMBL238
Ki 8.42 8.42 3.8 2
Sodium-dependent serotonin transporter
CHEMBL228
Ki 8.4 8.4 4.0 2
Sodium-dependent dopamine transporter
CHEMBL238
IC50 8.29 7.505 5.1 2
Cytochrome P450 2D6
CHEMBL289
IC50 6.1 6.1 800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sodium-dependent noradrenaline transporter Ki = 1.2 nM 8.92 Binding Assay: In order to evaluate the relative affinity of the various compoun... -
Sodium-dependent noradrenaline transporter Ki = 1.2 nM 8.92 Binding Assay: In order to evaluate the relative affinity of the various compoun... -
Sodium-dependent serotonin transporter IC50 = 1.7 nM 8.77 Displacement of [125I]-RTI-55 from recombinant SERT (unknown origin) expressed i... 25050161
Sodium-dependent noradrenaline transporter IC50 = 3.4 nM 8.47 Displacement of [125I]-RTI-55 from recombinant NET (unknown origin) expressed in... 25050161
Sodium-dependent dopamine transporter Ki = 3.8 nM 8.42 Binding Assay: In order to evaluate the relative affinity of the various compoun... -
Sodium-dependent dopamine transporter Ki = 3.8 nM 8.42 Binding Assay: In order to evaluate the relative affinity of the various compoun... -
Sodium-dependent serotonin transporter Ki = 4.0 nM 8.4 Binding Assay: In order to evaluate the relative affinity of the various compoun... -
Sodium-dependent serotonin transporter Ki = 4.0 nM 8.4 Binding Assay: In order to evaluate the relative affinity of the various compoun... -
Sodium-dependent dopamine transporter IC50 = 5.1 nM 8.29 Displacement of [125I]-RTI-55 from recombinant DAT (unknown origin) expressed in... 25050161
Sodium-dependent serotonin transporter IC50 = 69.0 nM 7.16 Displacement of [3H]Citolapram from human SERT expressed in HEK293E cells after ... 25050161
Sodium-dependent dopamine transporter IC50 = 190.0 nM 6.72 Displacement of [3H]WIN 35,428 from human DAT expressed in HEK293E cells after 1... 25050161
Sodium-dependent noradrenaline transporter IC50 = 350.0 nM 6.46 Displacement of [3H]Nisoxetine from human NET expressed in HEK293E cells after 1... 25050161
Cytochrome P450 2D6 IC50 = 800.0 nM 6.1 Inhibition of CYP2D6 (unknown origin) 25050161

Literature References

PubMed DOI Target Context # Activities
25050161 10.1021/ml500053b Sodium-dependent noradrenaline transporter 2
25050161 10.1021/ml500053b Sodium-dependent dopamine transporter 2
25050161 10.1021/ml500053b Sodium-dependent serotonin transporter 2
25050161 10.1021/ml500053b Cytochrome P450 2D6 1

Data from ChEMBL 36 via Core Engine