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Compound Detail

CHEMBL144901

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Cc1cccc2c(-c3ccc(F)cc3)cn(C3CCN(CCN4CCNC4=O)CC3)c12

Basic Information

ChEMBL ID CHEMBL144901
Phase Preclinical
Structure Type MOL
InChI Key BTXNBVXZBBDLMA-UHFFFAOYSA-N
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

420.5
MW (Da)
4.42
ALogP
3
HBA
1
HBD
40.5
PSA (Ų)
0.66
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 C25H29FN4O
MW 420.53
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.18

Activity Summary

IC50 5 meas. best 8.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serotonin 2 (5-HT2) receptor
CHEMBL2093870
IC50 8.44 8.44 3.6 2
Alpha-1A adrenergic receptor
CHEMBL319
IC50 7.64 7.64 23.0 1
D(2) dopamine receptor
CHEMBL339
IC50 6.43 6.43 370.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
1336054 10.1021/jm00104a007 Serotonin 2 (5-HT2) receptor 1
1336054 10.1021/jm00104a007 D(2) dopamine receptor 1
1336054 10.1021/jm00104a007 Alpha-1A adrenergic receptor 1
8151622 10.1021/jm00033a013 Serotonin 2 (5-HT2) receptor 1
8151622 10.1021/jm00033a013 D(2) dopamine receptor 1

Data from ChEMBL 36 via Core Engine