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Compound Detail

CHEMBL441259

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NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2[nH]nc3cc(F)ccc23)CC1

Basic Information

ChEMBL ID CHEMBL441259
Phase Preclinical
Structure Type MOL
InChI Key NPKCLZQNGLZUCO-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

420.5
MW (Da)
3.59
ALogP
4
HBA
2
HBD
84.2
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 C24H25FN4O2
MW 420.49
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.78

Activity Summary

Ki 5 meas. best 9.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent serotonin transporter
CHEMBL313
Ki 9.3 9.3 0.5 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 8.68 8.68 2.1 1
5-hydroxytryptamine receptor 1D
CHEMBL1983
Ki 7.62 7.62 24.0 1
D(2) dopamine receptor
CHEMBL339
Ki 7.48 7.48 33.0 1
5-hydroxytryptamine receptor 1B
CHEMBL1898
Ki 6.68 6.68 210.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15109634 10.1016/j.bmcl.2004.03.003 5-hydroxytryptamine receptor 1D 1
15109634 10.1016/j.bmcl.2004.03.003 5-hydroxytryptamine receptor 1B 1
15109634 10.1016/j.bmcl.2004.03.003 Sodium-dependent serotonin transporter 1
15109634 10.1016/j.bmcl.2004.03.003 Adrenergic receptor alpha-1 1
15109634 10.1016/j.bmcl.2004.03.003 D(2) dopamine receptor 1

Data from ChEMBL 36 via Core Engine