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Compound Detail

CHEMBL3394868

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COC(=O)N[C@H](C(=O)N1C[C@@H](C)C[C@H]1c1nc(-c2ccc(-c3ccc(-c4ccc5[nH]c([C@@H]6C[C@H](C)CN6C(=O)[C@@H](NC(=O)OC)C(C)C)nc5c4)cc3)cc2)c[nH]1)C(C)C

Basic Information

ChEMBL ID CHEMBL3394868
Phase Preclinical
Structure Type MOL
InChI Key UPGJLYYUAKKKAD-JVGMIBGKSA-N
0
Targets
2
Activities
1
Assay Types
6
PK Parameters
12
Publications
0
Known Names

Molecular Properties

817.0
MW (Da)
7.87
ALogP
8
HBA
4
HBD
174.6
PSA (Ų)
0.10
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C46H56N8O6
MW 817.00
Aromatic Rings 5
Heavy Atoms 60
NP-Likeness -0.46

Activity Summary

EC50 2 meas.

Pharmacokinetic Data

Parameter Value Units Species
AUC 2080.0 ng.hr.mL-1 Rattus norvegicus
CL 9.0 mL.min-1.kg-1 Rattus norvegicus
Cmax 0.03672 nM Rattus norvegicus
F 26.0 % Rattus norvegicus
T1/2 2.0 hr Rattus norvegicus
T1/2 3.5 hr Rattus norvegicus

Literature References

PubMed DOI Target Context # Activities
25577041 10.1016/j.bmcl.2014.12.045 Rattus norvegicus 7
25577041 10.1016/j.bmcl.2014.12.045 Hepatitis C virus 6
25577041 10.1016/j.bmcl.2014.12.045 ADMET 2
25577041 10.1016/j.bmcl.2014.12.045 Hepatocyte 2
25577041 10.1016/j.bmcl.2014.12.045 Voltage-gated inwardly rectifying potassium channel KCNH2 2
25577041 10.1016/j.bmcl.2014.12.045 Plasma 2
25577041 10.1016/j.bmcl.2014.12.045 Cytochrome P450 3A4 1
25577041 10.1016/j.bmcl.2014.12.045 Cytochrome P450 2C9 1
25577041 10.1016/j.bmcl.2014.12.045 Cytochrome P450 2D6 1
25577041 10.1016/j.bmcl.2014.12.045 Cytochrome P450 2C19 1
25577041 10.1016/j.bmcl.2014.12.045 Cytochrome P450 1A2 1
25577041 10.1016/j.bmcl.2014.12.045 MDCK 1

Data from ChEMBL 36 via Core Engine