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Compound Detail

CHEMBL4559333

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O=C(CCCOc1ccccc1)Nc1ncc(Cl)s1

Basic Information

ChEMBL ID CHEMBL4559333
Phase Preclinical
Structure Type MOL
InChI Key USCYPPPGRYWDHZ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
4
Publications
0
Known Names

Molecular Properties

296.8
MW (Da)
3.59
ALogP
4
HBA
1
HBD
51.2
PSA (Ų)
0.83
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H13ClN2O2S
MW 296.78
Aromatic Rings 2
Heavy Atoms 19
NP-Likeness -1.77

Activity Summary

EC50 1 meas. best 5.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein Tat
CHEMBL4011
EC50 5.3 5.3 5000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 90.0 mL.min-1.g-1 Homo sapiens
CL 814.0 mL.min-1.g-1 Mus musculus
T1/2 0.3167 hr Homo sapiens
T1/2 0.03333 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein Tat EC50 = 5000.0 nM 5.3 Activation of Tat-mediated HIV1 transcription in HEK293- FlpIn-FM cells harborin... 30973727

Literature References

PubMed DOI Target Context # Activities
30973727 10.1021/acs.jmedchem.9b00462 ADMET 4
30973727 10.1021/acs.jmedchem.9b00462 No relevant target 2
30973727 10.1021/acs.jmedchem.9b00462 Protein Tat 1
30973727 10.1021/acs.jmedchem.9b00462 HEK293 1

Data from ChEMBL 36 via Core Engine