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Compound Detail

CHEMBL4759180

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NC(N)=NCCCOc1ccc(C(=O)Nc2ccccc2Oc2ccccc2)cc1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL4759180
Phase Preclinical
Structure Type MOL
InChI Key YWJXVNMIVDKXDQ-UHFFFAOYSA-N
Parent Compound CHEMBL4803098
Active Moiety CHEMBL4803098
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

404.5
MW (Da)
3.77
ALogP
4
HBA
3
HBD
112.0
PSA (Ų)
0.29
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H25F3N4O5
MW 518.49
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.72

Activity Summary

IC50 2 meas. best 4.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Voltage-dependent T-type calcium channel subunit alpha-1H
CHEMBL1859
IC50 4.4 4.4 40000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32828422 10.1016/j.bmc.2020.115655 Voltage-dependent N-type calcium channel subunit alpha-1B 1
32828422 10.1016/j.bmc.2020.115655 Voltage-dependent T-type calcium channel subunit alpha-1H 1

Data from ChEMBL 36 via Core Engine