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Compound Detail

CHEMBL389237

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CO/N=C(\Cl)CCC/C=C(\c1cc(C)c(OC)c(/C(Cl)=N/OC)c1)c1cc(C)c2oc(=O)n(C)c2c1

Basic Information

ChEMBL ID CHEMBL389237
Phase Preclinical
Structure Type MOL
InChI Key DJXZJDRNSJSLQF-HFBMQGOESA-N
2
Targets
4
Activities
2
Assay Types
1
PK Parameters
12
Publications
0
Known Names

Molecular Properties

534.4
MW (Da)
6.10
ALogP
8
HBA
0
HBD
87.5
PSA (Ų)
0.18
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H29Cl2N3O5
MW 534.44
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.07

Activity Summary

EC50 2 meas. best 5.92
IC50 2 meas. best 6.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 reverse transcriptase
CHEMBL247
IC50 6.22 6.22 600.0 2
Human immunodeficiency virus 1
CHEMBL378
EC50 5.92 5.92 1200.0 2

Pharmacokinetic Data

Parameter Value Units Species
T1/2 82.83 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17579385 10.1021/jm070236e Human immunodeficiency virus 1 2
18083556 10.1016/j.bmcl.2007.11.114 Human immunodeficiency virus 1 2
17579385 10.1021/jm070236e Human immunodeficiency virus type 1 reverse transcriptase 1
17579385 10.1021/jm070236e Human immunodeficiency virus 2 1
17579385 10.1021/jm070236e CEM-SS 1
17579385 10.1021/jm070236e MT4 1
17579385 10.1021/jm070236e Plasma 1
18083556 10.1016/j.bmcl.2007.11.114 Human immunodeficiency virus 2 1
18083556 10.1016/j.bmcl.2007.11.114 Unchecked 1
18083556 10.1016/j.bmcl.2007.11.114 Human immunodeficiency virus type 1 reverse transcriptase 1
18083556 10.1016/j.bmcl.2007.11.114 CEM-SS 1
18083556 10.1016/j.bmcl.2007.11.114 MT4 1

Data from ChEMBL 36 via Core Engine