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Compound Detail

CHEMBL3310096

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CNC(=O)Cn1c(=O)c(C(=O)NCCOC)c(O)c2ncc(Cc3ccc(F)cc3)cc21

Basic Information

ChEMBL ID CHEMBL3310096
Phase Preclinical
Structure Type MOL
InChI Key TZMIHRDKFQXCPK-UHFFFAOYSA-N
2
Targets
5
Activities
1
Assay Types
9
PK Parameters
7
Publications
0
Known Names

Molecular Properties

442.4
MW (Da)
0.95
ALogP
7
HBA
3
HBD
122.5
PSA (Ų)
0.45
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23FN4O5
MW 442.45
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.15

Activity Summary

IC50 5 meas. best 8.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus
CHEMBL613758
IC50 8.64 8.2525 2.3 4
Human immunodeficiency virus type 1 integrase
CHEMBL3471
IC50 8.05 8.05 9.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 2.0 mL.min-1.kg-1 Macaca fascicularis
CL 13.8 mL.min-1.kg-1 Canis lupus familiaris
CL 0.5 mL.min-1.kg-1 Rattus norvegicus
F 19.0 % Macaca fascicularis
F 111.0 % Canis lupus familiaris
F 51.0 % Rattus norvegicus
T1/2 2.3 hr Macaca fascicularis
T1/2 1.2 hr Canis lupus familiaris
T1/2 3.7 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24908608 10.1016/j.bmcl.2014.05.011 Human immunodeficiency virus 6
24908608 10.1016/j.bmcl.2014.05.011 ADMET 3
24908608 10.1016/j.bmcl.2014.05.011 Cynomolgus monkey 3
24908608 10.1016/j.bmcl.2014.05.011 Canis familiaris 3
24908608 10.1016/j.bmcl.2014.05.011 Rattus norvegicus 3
24908608 10.1016/j.bmcl.2014.05.011 Cytochrome P450 1A2 1
24908608 10.1016/j.bmcl.2014.05.011 Human immunodeficiency virus type 1 integrase 1

Data from ChEMBL 36 via Core Engine