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Compound Detail

CHEMBL4096295

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CCOC(=O)C1=C(CN2CC(F)(F)C[C@@H]2CCC(=O)O)NC(c2nccs2)=N[C@H]1c1ccc(F)cc1Br

Basic Information

ChEMBL ID CHEMBL4096295
Phase Preclinical
Structure Type MOL
InChI Key UXFXZBOCQKBHLS-XOBRGWDASA-N
1
Targets
1
Activities
1
Assay Types
7
PK Parameters
4
Publications
0
Known Names

Molecular Properties

601.5
MW (Da)
4.53
ALogP
8
HBA
2
HBD
104.1
PSA (Ų)
0.41
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H24BrF3N4O4S
MW 601.45
Aromatic Rings 2
Heavy Atoms 37
NP-Likeness -0.81

Activity Summary

EC50 1 meas. best 7.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hepatitis B virus
CHEMBL613497
EC50 7.07 7.07 85.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 965.0 ng.hr.mL-1 Rattus norvegicus
AUC 999.0 ng.hr.mL-1 Rattus norvegicus
CL 21.0 mL.min-1.kg-1 Homo sapiens
CL 362.0 mL.min-1.kg-1 Mus musculus
CL 55.0 mL.min-1.kg-1 Canis lupus familiaris
CL 34.4 mL.min-1.kg-1 Rattus norvegicus
F 41.3 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Hepatitis B virus EC50 = 85.0 nM 7.07 Antiviral activity against HBV infected in human HepG2.2.15 replicon cells asses... 29381358

Literature References

PubMed DOI Target Context # Activities
29381358 10.1021/acs.jmedchem.7b01914 Rattus norvegicus 5
29381358 10.1021/acs.jmedchem.7b01914 Liver 3
29381358 10.1021/acs.jmedchem.7b01914 Hepatitis B virus 1
29381358 10.1021/acs.jmedchem.7b01914 Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine