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Compound Detail

CHEMBL307192

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CN1C(=O)N(C[C@@H](C(=O)NO)[C@@H](CC2CCCC2)C(=O)N2CCCCC2)C(=O)C1(C)C

Basic Information

ChEMBL ID CHEMBL307192
Phase Preclinical
Structure Type MOL
InChI Key GFUITADOEPNRML-IAGOWNOFSA-N

Known Names

Ro-32-3555
3
Targets
3
Activities
1
Assay Types
1
PK Parameters
6
Publications
1
Known Names

Molecular Properties

436.6
MW (Da)
1.99
ALogP
5
HBA
2
HBD
110.3
PSA (Ų)
0.36
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 C22H36N4O5
MW 436.55
Aromatic Rings 0
Heavy Atoms 31
NP-Likeness -0.28

Activity Summary

IC50 3 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Collagenase
CHEMBL2095216
IC50 8.15 8.15 7.0 1
Matrix metalloproteinase-9
CHEMBL321
IC50 7.23 7.23 59.0 1
Stromelysin-1
CHEMBL283
IC50 6.28 6.28 527.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 25.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Collagenase IC50 = 7.0 nM 8.15 Inhibition of human collagenase (MMP1) -
Matrix metalloproteinase-9 IC50 = 59.0 nM 7.23 Inhibition of human gelatinase B, MMP9 -
Stromelysin-1 IC50 = 527.0 nM 6.28 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