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Compound Detail

CHEMBL4439301

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Cc1cnc(NC(=O)CCCOc2cccc(Cl)c2)s1

Basic Information

ChEMBL ID CHEMBL4439301
Phase Preclinical
Structure Type MOL
InChI Key CKAGJBFFDLGXAM-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
5
Publications
0
Known Names

Molecular Properties

310.8
MW (Da)
3.90
ALogP
4
HBA
1
HBD
51.2
PSA (Ų)
0.82
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 C14H15ClN2O2S
MW 310.81
Aromatic Rings 2
Heavy Atoms 20
NP-Likeness -2.36

Activity Summary

EC50 1 meas. best 5.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein Tat
CHEMBL4011
EC50 5.89 5.89 1300.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 340.0 mL.min-1.g-1 Homo sapiens
CL 866.0 mL.min-1.g-1 Mus musculus
T1/2 0.08333 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 = 1300.0 nM 5.89 Activation of Tat-mediated HIV1 transcription in HEK293- FlpIn-FM cells harborin... 30973727

Literature References

Data from ChEMBL 36 via Core Engine