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Compound Detail

CHEMBL305729

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CC(C)C[C@@H](C(=O)N1CCCCC1)[C@@H](CN1C(=O)N(C)C(C)(C)C1=O)C(=O)NO

Basic Information

ChEMBL ID CHEMBL305729
Phase Preclinical
Structure Type MOL
InChI Key XNKSQYFVFJZMOA-HUUCEWRRSA-N
3
Targets
3
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

410.5
MW (Da)
1.46
ALogP
5
HBA
2
HBD
110.3
PSA (Ų)
0.38
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H34N4O5
MW 410.52
Aromatic Rings 0
Heavy Atoms 29
NP-Likeness -0.38

Activity Summary

IC50 3 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Collagenase
CHEMBL2095216
IC50 8.0 8.0 10.1 1
Matrix metalloproteinase-9
CHEMBL321
IC50 6.62 6.62 237.0 1
Stromelysin-1
CHEMBL283
IC50 5.66 5.66 2175.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 30.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Collagenase IC50 = 10.1 nM 8.0 Inhibition of human collagenase (MMP1) -
Matrix metalloproteinase-9 IC50 = 237.0 nM 6.62 Inhibition of human gelatinase B, MMP9 -
Stromelysin-1 IC50 = 2175.0 nM 5.66 Inhibition of human stromelysin-1, MMP-3 -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(97)00416-2 No relevant target 2
- 10.1016/S0960-894X(97)00416-2 Collagenase 1
- 10.1016/S0960-894X(97)00416-2 Stromelysin-1 1
- 10.1016/S0960-894X(97)00416-2 Matrix metalloproteinase-9 1
- 10.1016/S0960-894X(97)00416-2 ADMET 1
- 10.1016/S0960-894X(97)00416-2 Bos taurus 1

Data from ChEMBL 36 via Core Engine