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Compound Detail

CHEMBL494626

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CN1[C@H]2CC[C@@H]1[C@@H](C=C(Br)Br)[C@@H](c1ccc(Cl)cc1)C2.Cl

Basic Information

ChEMBL ID CHEMBL494626
Phase Preclinical
Structure Type MOL
InChI Key DNTKPSJIKIXCOA-VZXSFKIWSA-N
Parent Compound CHEMBL1187242
Active Moiety CHEMBL1187242
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

419.6
MW (Da)
5.54
ALogP
1
HBA
0
HBD
3.2
PSA (Ų)
0.61
QED
1
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H19Br2Cl2N
MW 456.05
Aromatic Rings 1
Heavy Atoms 20
NP-Likeness 0.34

Activity Summary

Ki 2 meas. best 8.46
IC50 1 meas. best 9.49

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent dopamine transporter
CHEMBL238
IC50 9.49 9.49 0.3 1
Sodium-dependent noradrenaline transporter
CHEMBL222
Ki 8.46 8.46 3.5 1
Sodium-dependent serotonin transporter
CHEMBL228
Ki 8.15 8.15 7.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18434164 10.1016/j.bmc.2008.04.008 Sodium-dependent dopamine transporter 1
18434164 10.1016/j.bmc.2008.04.008 Sodium-dependent noradrenaline transporter 1
18434164 10.1016/j.bmc.2008.04.008 Sodium-dependent serotonin transporter 1

Data from ChEMBL 36 via Core Engine