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Compound Detail

CHEMBL4125690

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CC1CCN(c2nc(C(F)(F)F)ccc2CNC(=O)C(C)c2cc(F)c(NS(C)(=O)=O)c(F)c2)CC1

Basic Information

ChEMBL ID CHEMBL4125690
Phase Preclinical
Structure Type MOL
InChI Key WIDHAOZPKVBNFE-UHFFFAOYSA-N
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

534.5
MW (Da)
4.41
ALogP
5
HBA
2
HBD
91.4
PSA (Ų)
0.51
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H27F5N4O3S
MW 534.55
Aromatic Rings 2
Heavy Atoms 36
NP-Likeness -1.48

Activity Summary

IC50 2 meas. best 8.09
Ki 2 meas. best 10.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Transient receptor potential cation channel subfamily V member 1
CHEMBL5102
Ki 10.0 10.0 0.1 1
Transient receptor potential cation channel subfamily V member 1
CHEMBL4794
Ki 9.7 9.7 0.2 1
Transient receptor potential cation channel subfamily V member 1
CHEMBL4794
IC50 8.09 8.075 8.1 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29884534 10.1016/j.bmcl.2018.05.043 Transient receptor potential cation channel subfamily V member 1 4
29884534 10.1016/j.bmcl.2018.05.043 Rattus norvegicus 2
29884534 10.1016/j.bmcl.2018.05.043 Mus musculus 2

Data from ChEMBL 36 via Core Engine