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Compound Detail

CHEMBL398201

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COc1c(C)cc(/C(=C/CCc2nnc(C)o2)c2cc(C)c3onc(OC)c3c2)cc1C(=O)SC

Basic Information

ChEMBL ID CHEMBL398201
Phase Preclinical
Structure Type MOL
InChI Key FDLCINKPCAWGRB-UFWORHAWSA-N
1
Targets
2
Activities
1
Assay Types
1
PK Parameters
12
Publications
0
Known Names

Molecular Properties

493.6
MW (Da)
5.72
ALogP
9
HBA
0
HBD
100.5
PSA (Ų)
0.30
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H27N3O5S
MW 493.59
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.51

Activity Summary

IC50 2 meas. best 4.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 reverse transcriptase
CHEMBL247
IC50 4.48 4.48 33000.0 2

Pharmacokinetic Data

Parameter Value Units Species
t1/2 - - Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17803290 10.1021/jm070382k Human immunodeficiency virus 1 2
18083556 10.1016/j.bmcl.2007.11.114 Human immunodeficiency virus 1 2
17803290 10.1021/jm070382k Human immunodeficiency virus type 1 reverse transcriptase 1
17803290 10.1021/jm070382k Human immunodeficiency virus 2 1
17803290 10.1021/jm070382k CEM-SS 1
17803290 10.1021/jm070382k MT4 1
17803290 10.1021/jm070382k 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