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Compound Detail

CHEMBL73763

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

Basic Information

ChEMBL ID CHEMBL73763
Phase Preclinical
Structure Type MOL
InChI Key OLEYZXUQGOKVKT-KFWWJZLASA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

469.6
MW (Da)
0.72
ALogP
6
HBA
4
HBD
148.2
PSA (Ų)
0.22
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H39N5O6
MW 469.58
Aromatic Rings 0
Heavy Atoms 33
NP-Likeness 0.13

Activity Summary

IC50 2 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Collagenase
CHEMBL2095216
IC50 9.0 9.0 1.0 1
Matrix metalloproteinase-9
CHEMBL321
IC50 8.55 8.55 2.8 1

Pharmacokinetic Data

Parameter Value Units Species
F 1.5 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Collagenase IC50 = 1.0 nM 9.0 Inhibition of human collagenase (MMP1) -
Matrix metalloproteinase-9 IC50 = 2.8 nM 8.55 Inhibition of human gelatinase B, MMP9 -

Literature References

PubMed DOI Target Context # Activities
- 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 No relevant target 1
- 10.1016/S0960-894X(97)00416-2 ADMET 1

Data from ChEMBL 36 via Core Engine