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Compound Detail

CHEMBL144457

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CNC(=O)N(C)CCN1CCC(c2cn(-c3ccc(F)cc3)c3cc(Cl)ccc23)CC1

Basic Information

ChEMBL ID CHEMBL144457
Phase Preclinical
Structure Type MOL
InChI Key RGLSIOAWUHXTFV-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

443.0
MW (Da)
4.87
ALogP
3
HBA
1
HBD
40.5
PSA (Ų)
0.61
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H28ClFN4O
MW 442.97
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.49

Activity Summary

IC50 3 meas. best 8.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serotonin 2 (5-HT2) receptor
CHEMBL2093870
IC50 8.8 8.8 1.6 1
Adrenergic receptor alpha-1
CHEMBL1907610
IC50 7.8 7.8 16.0 1
D(2) dopamine receptor
CHEMBL339
IC50 7.09 7.09 82.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
1336053 10.1021/jm00104a006 Rattus norvegicus 4
1336053 10.1021/jm00104a006 Mus musculus 2
1336053 10.1021/jm00104a006 Serotonin 2 (5-HT2) receptor 1
1336053 10.1021/jm00104a006 D(2) dopamine receptor 1
1336053 10.1021/jm00104a006 Adrenergic receptor alpha-1 1

Data from ChEMBL 36 via Core Engine