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Compound Detail

CHEMBL272603

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S=c1sc2ccccc2n1CCCCN1CCN(C2CCCCC2)CC1

Basic Information

ChEMBL ID CHEMBL272603
Phase Preclinical
Structure Type MOL
InChI Key FJGOTAJCEJCFEV-UHFFFAOYSA-N
8
Targets
15
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

389.6
MW (Da)
5.16
ALogP
5
HBA
0
HBD
11.4
PSA (Ų)
0.50
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H31N3S2
MW 389.63
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -1.57

Activity Summary

Ki 15 meas. best 9.26

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 9.26 8.6283 0.6 6
Sigma non-opioid intracellular receptor 1
CHEMBL3602
Ki 8.89 8.89 1.3 3
D(2) dopamine receptor
CHEMBL217
Ki 5.98 5.98 1041.0 1
D(2) dopamine receptor
CHEMBL339
Ki 5.98 5.98 1041.0 1
Sodium-dependent dopamine transporter
CHEMBL238
Ki 5.93 5.93 1175.0 1
Sodium-dependent dopamine transporter
CHEMBL338
Ki 5.93 5.93 1175.0 1
Sodium-dependent serotonin transporter
CHEMBL228
Ki 5.85 5.85 1402.0 1
Sodium-dependent serotonin transporter
CHEMBL313
Ki 5.85 5.85 1402.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked Ki = 0.55 nM 9.26 Displacement of [3H]DTG from opioid sigma2 receptor in rat brain homogenate 18278854
Unchecked Ki = 0.55 nM 9.26 Receptor Assay: Compounds were evaluated for σ-1 and σ-2 binding in rat brain ho... -
Unchecked Ki = 0.55 nM 9.26 Receptor Assay: Compounds were evaluated for σ-1 and σ-2 binding in rat brain ho... -
Unchecked Ki = 0.6 nM 9.22 Displacement of [3H]DTG from sigma2 receptor in rat brain homogenate in presence... 22850210
Sigma non-opioid intracellular receptor 1 Ki = 1.28 nM 8.89 Displacement of [3H](+)-pentazocine from opioid sigma1 receptor in rat brain hom... 18278854
Sigma non-opioid intracellular receptor 1 Ki = 1.3 nM 8.89 Displacement of [3H](+)-pentazocine from sigma1 receptor in rat brain homogenate... 22850210
Unchecked Ki = 1.28 nM 8.89 Receptor Assay: Compounds were evaluated for σ-1 and σ-2 binding in rat brain ho... -
Sigma non-opioid intracellular receptor 1 Ki = 1.28 nM 8.89 Receptor Assay: Compounds were evaluated for σ-1 and σ-2 binding in rat brain ho... -
D(2) dopamine receptor Ki = 1041.0 nM 5.98 Displacement of [3H](-)-sulpiride from dopamine D2 receptor in rat brain homogen... 18278854
D(2) dopamine receptor Ki = 1041.0 nM 5.98 Receptor Assay: Compounds were evaluated for σ-1 and σ-2 binding in rat brain ho... -
Sodium-dependent dopamine transporter Ki = 1175.0 nM 5.93 Displacement of [3H]WIN-35428 from dopamine transporter in rat brain homogenate 18278854
Sodium-dependent dopamine transporter Ki = 1175.0 nM 5.93 Receptor Assay: Compounds were evaluated for σ-1 and σ-2 binding in rat brain ho... -
Unchecked Ki = 1326.0 nM 5.88 Displacement of [3H]ketanserin from 5HT2 receptor in rat brain homogenate 18278854
Sodium-dependent serotonin transporter Ki = 1402.0 nM 5.85 Displacement of [3H]paroxetine from serotonin transporter in rat brain homogenat... 18278854
Sodium-dependent serotonin transporter Ki = 1402.0 nM 5.85 Receptor Assay: Compounds were evaluated for σ-1 and σ-2 binding in rat brain ho... -

Literature References

PubMed DOI Target Context # Activities
18278854 10.1021/jm701357m Unchecked 4
18278854 10.1021/jm701357m Sigma non-opioid intracellular receptor 1 1
18278854 10.1021/jm701357m Sodium-dependent dopamine transporter 1
18278854 10.1021/jm701357m Sodium-dependent serotonin transporter 1
18278854 10.1021/jm701357m Norepinephrine transporter 1
18278854 10.1021/jm701357m Glutamate NMDA receptor 1
18278854 10.1021/jm701357m D(2) dopamine receptor 1
22850210 10.1016/j.bmcl.2012.07.026 Sigma non-opioid intracellular receptor 1 1
22850210 10.1016/j.bmcl.2012.07.026 Unchecked 1

Data from ChEMBL 36 via Core Engine