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Compound Detail

CHEMBL4847626

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CN1CCC(=C(F)c2cccc(NC(=O)c3ccc(F)cc3F)n2)CC1

Basic Information

ChEMBL ID CHEMBL4847626
Phase Preclinical
Structure Type MOL
InChI Key MHGKBBQGVRMHIQ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
8
PK Parameters
2
Publications
0
Known Names

Molecular Properties

361.4
MW (Da)
4.02
ALogP
3
HBA
1
HBD
45.2
PSA (Ų)
0.90
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H18F3N3O
MW 361.37
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -1.58

Activity Summary

IC50 1 meas. best 8.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1F
CHEMBL1805
IC50 8.33 8.33 4.7 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 70.4 ng.hr.mL-1 Rattus norvegicus
AUC 44.6 ng.hr.mL-1 Rattus norvegicus
CL 229.0 mL.min-1.kg-1 Rattus norvegicus
Cmax 205.88 nM Rattus norvegicus
Cmax 26.87 nM Rattus norvegicus
F 12.9 % Rattus norvegicus
T1/2 1.05 hr Rattus norvegicus
T1/2 0.824 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34419891 10.1016/j.ejmech.2021.113782 ADMET 9
34419891 10.1016/j.ejmech.2021.113782 5-hydroxytryptamine receptor 1F 2

Data from ChEMBL 36 via Core Engine