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Compound Detail

CHEMBL511555

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N[C@@H](CN1CCN(c2nc3cc(F)ccc3n3cccc23)CC1)C(=O)O

Basic Information

ChEMBL ID CHEMBL511555
Phase Preclinical
Structure Type MOL
InChI Key CTKOQDQPYZTIFY-ZDUSSCGKSA-N
3
Targets
3
Activities
1
Assay Types
2
PK Parameters
12
Publications
0
Known Names

Molecular Properties

357.4
MW (Da)
1.16
ALogP
6
HBA
2
HBD
87.1
PSA (Ų)
0.73
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H20FN5O2
MW 357.39
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -1.42

Activity Summary

Ki 3 meas. best 8.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 3A
CHEMBL2411
Ki 8.55 8.55 2.8 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 6.35 6.35 446.0 1
5-hydroxytryptamine receptor 2A
CHEMBL322
Ki 5.25 5.25 5692.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 90.0 mL.min-1.kg-1 Mus musculus
T1/2 0.8833 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19425598 10.1021/jm900018b 5-hydroxytryptamine receptor 3A 5
19425598 10.1021/jm900018b Mus musculus 5
19425598 10.1021/jm900018b Brain 4
19425598 10.1021/jm900018b Rattus norvegicus 2
19425598 10.1021/jm900018b 5-hydroxytryptamine receptor 1A 1
19425598 10.1021/jm900018b 5-hydroxytryptamine receptor 2A 1
19425598 10.1021/jm900018b 5-hydroxytryptamine receptor 4 1
19425598 10.1021/jm900018b Adrenergic receptor alpha-1 1
19425598 10.1021/jm900018b Alpha-2A adrenergic receptor 1
19425598 10.1021/jm900018b D(1A) dopamine receptor 1
19425598 10.1021/jm900018b D(2) dopamine receptor 1
19425598 10.1021/jm900018b Muscarinic acetylcholine receptor 1

Data from ChEMBL 36 via Core Engine