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Compound Detail

CHEMBL373731

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Nc1ncc2cccc(Oc3cc(-c4ccc(C(F)(F)F)cc4)ncn3)c2n1

Basic Information

ChEMBL ID CHEMBL373731
Phase Preclinical
Structure Type MOL
InChI Key HEWLFIQAUUHYHC-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
3
Publications
0
Known Names

Molecular Properties

383.3
MW (Da)
4.48
ALogP
6
HBA
1
HBD
86.8
PSA (Ų)
0.56
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H12F3N5O
MW 383.33
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -1.17

Activity Summary

IC50 1 meas. best 7.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Transient receptor potential cation channel subfamily V member 1
CHEMBL5102
IC50 7.85 7.85 14.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 14.0 mL.min-1.g-1 Homo sapiens
CL 38.0 mL.min-1.g-1 Rattus norvegicus
CL 25.0 mL.min-1.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17585750 10.1021/jm070190p Transient receptor potential cation channel subfamily V member 1 2
17585750 10.1021/jm070190p Liver microsomes 2
17585750 10.1021/jm070190p Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine