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Compound Detail

CHEMBL116195

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CN1C2CCC1C(c1nnc(-c3ccccc3)o1)C(c1ccc(Cl)cc1)C2

Basic Information

ChEMBL ID CHEMBL116195
Phase Preclinical
Structure Type MOL
InChI Key BTMJKIPIYJYOOV-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

379.9
MW (Da)
5.12
ALogP
4
HBA
0
HBD
42.2
PSA (Ų)
0.63
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H22ClN3O
MW 379.89
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.54

Activity Summary

IC50 3 meas. best 7.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent dopamine transporter
CHEMBL338
IC50 7.9 7.9 12.6 1
Norepinephrine transporter
CHEMBL304
IC50 6.03 6.03 929.0 1
Sodium-dependent serotonin transporter
CHEMBL313
IC50 5.48 5.48 3300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
7658431 10.1021/jm00018a004 Sodium-dependent dopamine transporter 1
7658431 10.1021/jm00018a004 Norepinephrine transporter 1
7658431 10.1021/jm00018a004 Sodium-dependent serotonin transporter 1
7658431 10.1021/jm00018a004 Unchecked 1
7658431 10.1021/jm00018a004 Monoamine transporters; serotonin & dopamine 1

Data from ChEMBL 36 via Core Engine