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Compound Detail

CHEMBL244998

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COc1c(C)cc(/C(=C\CCc2nnc(C)o2)c2cccc(C#N)c2)cc1C(=O)SC

Basic Information

ChEMBL ID CHEMBL244998
Phase Preclinical
Structure Type MOL
InChI Key RBDGPWIWHUSKOE-UKWGHVSLSA-N
2
Targets
2
Activities
2
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 -0.88

Activity Summary

EC50 1 meas. best 5.85
IC50 1 meas. best 5.03

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus 1
CHEMBL378
EC50 5.85 5.85 1400.0 1
Human immunodeficiency virus type 1 reverse transcriptase
CHEMBL247
IC50 5.03 5.03 9300.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 3.683 hr 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
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

Data from ChEMBL 36 via Core Engine