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Compound Detail

CHEMBL284134

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CC(C)NC(=O)OCc1c(COC(=O)NC(C)C)c(-c2ccc(Cl)c(Cl)c2)n2c1CCC2

Basic Information

ChEMBL ID CHEMBL284134
Phase Preclinical
Structure Type MOL
InChI Key CCBHSPUYWZHDFX-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
15
PK Parameters
10
Publications
0
Known Names

Molecular Properties

482.4
MW (Da)
5.68
ALogP
5
HBA
2
HBD
81.6
PSA (Ų)
0.53
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 C23H29Cl2N3O4
MW 482.41
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -0.69

Activity Summary

IC50 3 meas. best 5.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HL-60
CHEMBL383
IC50 5.82 5.82 1500.0 1
Cytochrome P450 2D6
CHEMBL289
IC50 4.96 4.96 11000.0 1

Pharmacokinetic Data

Parameter Value Units Species
KE 0.8 - Mus musculus
KE - - Mus musculus
KE 6.68 - Mus musculus
KE 4.35 - Mus musculus
KE 5.71 - Mus musculus
KE 5.27 - Mus musculus
KE 2.81 - Mus musculus
KE 3.01 - Mus musculus
KE 1.85 - Mus musculus
KE 1.4 - Mus musculus
KE 1.08 - Mus musculus
KE -0.07 - Mus musculus
KE 0.69 - Mus musculus
KE -0.55 - Mus musculus
T1/2 0.2167 hr -

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
3669018 10.1021/jm00394a030 NON-PROTEIN TARGET 44
6887210 10.1021/jm00363a023 P388 33
3669018 10.1021/jm00394a030 P388 12
7086826 10.1021/jm00343a017 Mus musculus 9
3669018 10.1021/jm00394a030 Unchecked 3
6887210 10.1021/jm00363a023 ADMET 2
3164410 10.1021/jm00402a030 HL-60 2
15481972 10.1021/jm049934e Cytochrome P450 2D6 1
18834112 10.1021/jm800656v Amine oxidase [flavin-containing] A 1
24095754 10.1016/j.ejmech.2013.09.016 HL-60 1

Data from ChEMBL 36 via Core Engine