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Compound Detail

CHEMBL520035

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CN1C2CCC1[C@@H](c1cc(Cc3ccc(Cl)cc3)no1)[C@@H](c1ccc(Cl)cc1)C2.Cl

Basic Information

ChEMBL ID CHEMBL520035
Phase Preclinical
Structure Type MOL
InChI Key IRDYKJUJFKVPBO-LIAHKDQHSA-N
Parent Compound CHEMBL1187773
Active Moiety CHEMBL1187773
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

427.4
MW (Da)
6.31
ALogP
3
HBA
0
HBD
29.3
PSA (Ų)
0.49
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H25Cl3N2O
MW 463.84
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.31

Activity Summary

Ki 2 meas. best 7.1
IC50 1 meas. best 7.76

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent dopamine transporter
CHEMBL238
IC50 7.76 7.76 17.5 1
Sodium-dependent serotonin transporter
CHEMBL228
Ki 7.1 7.1 79.0 1
Sodium-dependent noradrenaline transporter
CHEMBL222
Ki 6.17 6.17 677.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18556210 10.1016/j.bmc.2008.05.073 Sodium-dependent dopamine transporter 1
18556210 10.1016/j.bmc.2008.05.073 Sodium-dependent noradrenaline transporter 1
18556210 10.1016/j.bmc.2008.05.073 Sodium-dependent serotonin transporter 1

Data from ChEMBL 36 via Core Engine