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Compound Detail

CHEMBL4865700

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

Basic Information

ChEMBL ID CHEMBL4865700
Phase Preclinical
Structure Type MOL
InChI Key TWNUOOXNMMOWRI-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
8
PK Parameters
2
Publications
0
Known Names

Molecular Properties

377.8
MW (Da)
4.53
ALogP
3
HBA
1
HBD
45.2
PSA (Ų)
0.85
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 C19H18ClF2N3O
MW 377.82
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -1.64

Activity Summary

IC50 1 meas. best 7.63

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1F
CHEMBL1805
IC50 7.63 7.63 23.4 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 90.5 ng.hr.mL-1 Rattus norvegicus
AUC 105.0 ng.hr.mL-1 Rattus norvegicus
CL 178.0 mL.min-1.kg-1 Rattus norvegicus
Cmax 191.1 nM Rattus norvegicus
Cmax 61.4 nM Rattus norvegicus
F 26.2 % Rattus norvegicus
T1/2 1.42 hr Rattus norvegicus
T1/2 1.68 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