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Compound Detail

CHEMBL230966

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COc1c(C)cc(/C(=C/CCc2nnc(C)o2)c2ccc(C#N)cc2)cc1C(=O)SC

Basic Information

ChEMBL ID CHEMBL230966
Phase Preclinical
Structure Type MOL
InChI Key HIKJWXOTYYTOFH-CGOBSMCZSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

433.5
MW (Da)
5.13
ALogP
7
HBA
0
HBD
89.0
PSA (Ų)
0.51
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H23N3O3S
MW 433.53
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.78

Activity Summary

IC50 1 meas. best 4.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 reverse transcriptase
CHEMBL247
IC50 4.32 4.32 48000.0 1

Pharmacokinetic Data

Parameter Value Units Species
t1/2 - - Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Human immunodeficiency virus type 1 reverse transcriptase IC50 = 48000.0 nM 4.32 Inhibition of HIV1 reverse transcriptase 17803290

Literature References

PubMed DOI Target Context # Activities
17803290 10.1021/jm070382k Human immunodeficiency virus 1 2
17803290 10.1021/jm070382k Human immunodeficiency virus 2 1
17803290 10.1021/jm070382k Human immunodeficiency virus type 1 reverse transcriptase 1
17803290 10.1021/jm070382k CEM-SS 1
17803290 10.1021/jm070382k MT4 1
17803290 10.1021/jm070382k Plasma 1

Data from ChEMBL 36 via Core Engine