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Compound Detail

CHEMBL522699

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CN1[C@H]2CC[C@@H]1[C@@H](C#Cc1ccc([N+](=O)[O-])cc1)[C@@H](c1ccc(Cl)cc1)C2.Cl

Basic Information

ChEMBL ID CHEMBL522699
Phase Preclinical
Structure Type MOL
InChI Key XFRJSOUJVWXXAT-GAPKJMMISA-N
Parent Compound CHEMBL1187818
Active Moiety CHEMBL1187818
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

380.9
MW (Da)
4.87
ALogP
3
HBA
0
HBD
46.4
PSA (Ų)
0.42
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H22Cl2N2O2
MW 417.34
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.47

Activity Summary

Ki 2 meas. best 6.64
IC50 1 meas. best 9.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent dopamine transporter
CHEMBL238
IC50 9.05 9.05 0.9 1
Sodium-dependent noradrenaline transporter
CHEMBL222
Ki 6.64 6.64 230.0 1
Sodium-dependent serotonin transporter
CHEMBL228
Ki 6.21 6.21 620.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18434164 10.1016/j.bmc.2008.04.008 Unchecked 2
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