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Compound Detail

CHEMBL227228

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Nc1nc2c(Oc3cc(-c4ccc(C(F)(F)F)cc4)ncn3)cccc2s1

Basic Information

ChEMBL ID CHEMBL227228
Phase Preclinical
Structure Type MOL
InChI Key IUSOBMHCOYGJSN-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
3
Publications
0
Known Names

Molecular Properties

388.4
MW (Da)
5.15
ALogP
6
HBA
1
HBD
73.9
PSA (Ų)
0.53
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H11F3N4OS
MW 388.37
Aromatic Rings 4
Heavy Atoms 27
NP-Likeness -1.68

Activity Summary

IC50 1 meas. best 8.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Transient receptor potential cation channel subfamily V member 1
CHEMBL5102
IC50 8.92 8.92 1.2 1

Pharmacokinetic Data

Parameter Value Units Species
CL 5.0 mL.min-1.g-1 Homo sapiens
CL 47.0 mL.min-1.g-1 Rattus norvegicus
CL 3.667 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