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Compound Detail

CHEMBL551051

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O=C(N[C@@H]1CCCc2c1[nH]c1ccc(Cl)cc21)c1ccccn1

Basic Information

ChEMBL ID CHEMBL551051
Phase Preclinical
Structure Type MOL
InChI Key WJQBOBGVBBZLJU-OAHLLOKOSA-N
3
Targets
3
Activities
2
Assay Types
9
PK Parameters
11
Publications
0
Known Names

Molecular Properties

325.8
MW (Da)
4.02
ALogP
2
HBA
2
HBD
57.8
PSA (Ų)
0.75
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H16ClN3O
MW 325.80
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -1.07

Activity Summary

IC50 2 meas. best 8.3
Ki 1 meas. best 6.69

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human papillomavirus type 16
CHEMBL613205
IC50 8.3 8.3 5.0 1
Dengue virus
CHEMBL613757
IC50 7.88 7.88 13.3 1
Dihydroorotate dehydrogenase (quinone), mitochondrial
CHEMBL1966
Ki 6.69 6.69 203.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 13.1 mL.min-1.kg-1 Rattus norvegicus
CL 5.0 mL.min-1.kg-1 Canis lupus familiaris
CL 1.1 mL.min-1.kg-1 Macaca mulatta
F 56.0 % Rattus norvegicus
F 35.0 % Canis lupus familiaris
F 56.0 % Macaca mulatta
T1/2 4.1 hr Rattus norvegicus
T1/2 9.5 hr Canis lupus familiaris
T1/2 3.6 hr Macaca mulatta

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19556128 10.1016/j.bmcl.2009.06.001 Rattus norvegicus 4
19556128 10.1016/j.bmcl.2009.06.001 Canis familiaris 4
19556128 10.1016/j.bmcl.2009.06.001 Rhesus monkey 4
19556128 10.1016/j.bmcl.2009.06.001 Unchecked 2
19556128 10.1016/j.bmcl.2009.06.001 Human papillomavirus type 16 1
19556128 10.1016/j.bmcl.2009.06.001 HFF 1
19556128 10.1016/j.bmcl.2009.06.001 Cytochrome P450 2D6 1
19556128 10.1016/j.bmcl.2009.06.001 Voltage-gated inwardly rectifying potassium channel KCNH2 1
31420268 10.1016/j.bmcl.2019.08.010 Dihydroorotate dehydrogenase (quinone), mitochondrial 1
31557612 10.1016/j.ejmech.2019.111681 Dihydroorotate dehydrogenase (quinone), mitochondrial 1
31557612 10.1016/j.ejmech.2019.111681 Dengue virus 1

Data from ChEMBL 36 via Core Engine