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Compound Detail

CHEMBL1237325

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O.O=c1[nH]c2ccccc2c(=O)n1CCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1

Basic Information

ChEMBL ID CHEMBL1237325
Phase Preclinical
Structure Type MOL
InChI Key UTURDBDABVHOPB-UHFFFAOYSA-N
Parent Compound CHEMBL305690
Active Moiety CHEMBL305690
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

502.6
MW (Da)
3.86
ALogP
5
HBA
1
HBD
61.3
PSA (Ų)
0.45
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H30F2N4O3
MW 520.58
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -0.71

Activity Summary

IC50 3 meas. best 8.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serotonin 2 (5-HT2) receptor
CHEMBL2093870
IC50 8.54 8.54 2.9 1
Adrenergic receptor alpha-1
CHEMBL1907610
IC50 8.28 8.28 5.3 1
D(2) dopamine receptor
CHEMBL339
IC50 7.72 7.72 19.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2903929 10.1021/jm00120a003 Rattus norvegicus 8
2903929 10.1021/jm00120a003 Mus musculus 1
2903929 10.1021/jm00120a003 Serotonin 2 (5-HT2) receptor 1
2903929 10.1021/jm00120a003 D(2) dopamine receptor 1
2903929 10.1021/jm00120a003 Adrenergic receptor alpha-1 1

Data from ChEMBL 36 via Core Engine