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Compound Detail

CHEMBL4788669

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COc1cc(-c2noc([C@H](C)NC(=O)c3cc(C(F)(F)F)nn3C)n2)ccn1

Basic Information

ChEMBL ID CHEMBL4788669
Phase Preclinical
Structure Type MOL
InChI Key HBUQPGAOVFRJMM-QMMMGPOBSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

396.3
MW (Da)
2.38
ALogP
8
HBA
1
HBD
108.0
PSA (Ų)
0.71
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H15F3N6O3
MW 396.33
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -2.23

Activity Summary

IC50 2 meas. best 7.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Potassium channel subfamily T member 1
CHEMBL4739688
IC50 7.57 7.57 27.0 1
Potassium channel subfamily T member 1
CHEMBL4739694
IC50 5.52 5.52 3001.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 9.6 mL.min-1.g-1 Not specified

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33859800 10.1021/acsmedchemlett.0c00675 Potassium channel subfamily T member 1 2
33859800 10.1021/acsmedchemlett.0c00675 No relevant target 2
33859800 10.1021/acsmedchemlett.0c00675 ADMET 1

Data from ChEMBL 36 via Core Engine