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Compound Detail

CHEMBL4446551

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CC(C)CCN1C(=O)[C@]2(CC(=O)Nc3c2nnn3[C@@H](C)c2ccc(Cl)cc2)c2cc(Cl)ccc21

Basic Information

ChEMBL ID CHEMBL4446551
Phase Preclinical
Structure Type MOL
InChI Key UCOQXTLXEBGWHG-ODCWNRFASA-N
3
Targets
7
Activities
1
Assay Types
12
PK Parameters
6
Publications
0
Known Names

Molecular Properties

498.4
MW (Da)
5.22
ALogP
5
HBA
1
HBD
80.1
PSA (Ų)
0.52
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H25Cl2N5O2
MW 498.41
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.96

Activity Summary

EC50 7 meas. best 7.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
dengue virus type 3
CHEMBL612717
EC50 7.46 7.46 35.0 1
dengue virus type 2
CHEMBL613966
EC50 7.0 6.662 100.0 5
dengue virus type 1
CHEMBL613360
EC50 6.11 6.11 780.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 6240.0 ng.hr.mL-1 Rattus norvegicus
AUC 10334.0 ng.hr.mL-1 Rattus norvegicus
CL 59.5 mL.min-1.kg-1 Rattus norvegicus
CL 13.67 mL.min-1.kg-1 Rattus norvegicus
Cmax 3043.68 nM Rattus norvegicus
Cmax 20725.91 nM Rattus norvegicus
F 30.0 % Rattus norvegicus
MRT 3.46 hr Rattus norvegicus
MRT 2.28 hr Rattus norvegicus
T1/2 2.24 hr Rattus norvegicus
T1/2 2.29 hr Rattus norvegicus
Tmax 1.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31403780 10.1021/acs.jmedchem.9b00698 ADMET 14
31403780 10.1021/acs.jmedchem.9b00698 dengue virus type 2 8
31403780 10.1021/acs.jmedchem.9b00698 dengue virus type 1 1
31403780 10.1021/acs.jmedchem.9b00698 dengue virus type 3 1
31403780 10.1021/acs.jmedchem.9b00698 dengue virus type 4 1
31403780 10.1021/acs.jmedchem.9b00698 Huh-7 1

Data from ChEMBL 36 via Core Engine