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Compound Detail

CHEMBL4064672

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COC(=O)C1=C(CN2CCOC[C@H]2C(=O)O)NC(c2nccs2)=N[C@H]1c1ccc(F)cc1Cl

Basic Information

ChEMBL ID CHEMBL4064672
Phase Preclinical
Structure Type MOL
InChI Key QJLRUAVQNXTCMO-RDJZCZTQSA-N
2
Targets
4
Activities
1
Assay Types
9
PK Parameters
20
Publications
0
Known Names

Molecular Properties

494.9
MW (Da)
2.24
ALogP
9
HBA
2
HBD
113.3
PSA (Ų)
0.59
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H20ClFN4O5S
MW 494.93
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.21

Activity Summary

EC50 4 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Core antigen
CHEMBL1075091
EC50 8.52 8.52 3.0 1
Hepatitis B virus
CHEMBL613497
EC50 8.52 8.4533 3.0 3

Pharmacokinetic Data

Parameter Value Units Species
AUC 878.0 ng.hr.mL-1 Mus musculus
AUC 962.0 ng.hr.mL-1 Mus musculus
AUC 11800.0 ng.hr.mL-1 Mus musculus
CL 19.0 mL.min-1.kg-1 Mus musculus
Cmax 834.46 nM Mus musculus
F 37.0 % Mus musculus
Fu 0.057 - Homo sapiens
Fu 0.074 - Mus musculus
T1/2 1.5 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28339215 10.1021/acs.jmedchem.7b00083 No relevant target 6
28339215 10.1021/acs.jmedchem.7b00083 Mus musculus 6
29381358 10.1021/acs.jmedchem.7b01914 Hepatitis B virus 5
28339215 10.1021/acs.jmedchem.7b00083 Hepatitis B virus 3
28339215 10.1021/acs.jmedchem.7b00083 Plasma 3
29381358 10.1021/acs.jmedchem.7b01914 Unchecked 3
29381358 10.1021/acs.jmedchem.7b01914 Cytochrome P450 3A4 3
36896968 10.1021/acs.jmedchem.3c00173 Unchecked 2
28339215 10.1021/acs.jmedchem.7b00083 Unchecked 2
31689116 10.1021/acs.jmedchem.9b01421 Unchecked 2
28339215 10.1021/acs.jmedchem.7b00083 Cytochrome P450 3A4 2
28339215 10.1021/acs.jmedchem.7b00083 Voltage-gated inwardly rectifying potassium channel KCNH2 2
28339215 10.1021/acs.jmedchem.7b00083 Cytochrome P450 2D6 1
28339215 10.1021/acs.jmedchem.7b00083 Cytochrome P450 2C9 1
28339215 10.1021/acs.jmedchem.7b00083 Cytochrome P450 2C19 1
28339215 10.1021/acs.jmedchem.7b00083 Cytochrome P450 1A2 1
28339215 10.1021/acs.jmedchem.7b00083 Hepatocyte 1
29381358 10.1021/acs.jmedchem.7b01914 Voltage-gated inwardly rectifying potassium channel KCNH2 1
28339215 10.1021/acs.jmedchem.7b00083 Salmonella typhimurium 1
28339215 10.1021/acs.jmedchem.7b00083 ADMET 1

Data from ChEMBL 36 via Core Engine