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Compound Detail

CHEMBL4445882

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C[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)COCCOCCNC(=O)CCOCCOCCOCCNC(=O)CCc1ccc(C(=C\C=C2\N(CCCCS(=O)(=O)O)c3ccc4c(S(=O)(=O)[O-])cc(S(=O)(=O)O)cc4c3C2(C)C)/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccc4c(S(=O)(=O)O)cc(S(=O)(=O)O)cc4c3C2(C)C)cc1)P(=O)(O)C[C@@H](CCc1ccccc1)C(=O)O

Basic Information

ChEMBL ID CHEMBL4445882
Phase Preclinical
Structure Type MOL
InChI Key RUVHVYMIMBVNKN-YQGUEOHTSA-N
8
Targets
10
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

1974.2
MW (Da)

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C87H109N6O32PS6
MW 1974.22

Activity Summary

Ki 10 meas. best 10.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mast cell carboxypeptidase A
CHEMBL4523202
Ki 10.77 10.77 0.0 1
Carboxypeptidase A1
CHEMBL2088
Ki 10.15 9.94 0.1 3
Carboxypeptidase A2
CHEMBL4939
Ki 8.28 8.28 5.3 1
Carboxypeptidase A4
CHEMBL2644
Ki 8.24 8.24 5.7 1
Collagenase 3
CHEMBL280
Ki 6.25 6.25 562.0 1
Stromelysin-2
CHEMBL4270
Ki 6.01 6.01 983.0 1
Macrophage metalloelastase
CHEMBL4393
Ki 5.87 5.87 1340.0 1
Matrix metalloproteinase-9
CHEMBL321
Ki 5.59 5.59 2588.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30688452 10.1021/acs.jmedchem.8b01465 Carboxypeptidase A1 5
30688452 10.1021/acs.jmedchem.8b01465 Mast cell carboxypeptidase A 2
30688452 10.1021/acs.jmedchem.8b01465 Unchecked 2
30688452 10.1021/acs.jmedchem.8b01465 Prothrombin 1
30688452 10.1021/acs.jmedchem.8b01465 Carboxypeptidase B2 1
30688452 10.1021/acs.jmedchem.8b01465 Carboxypeptidase N catalytic chain 1
30688452 10.1021/acs.jmedchem.8b01465 Cytosolic carboxypeptidase 1 1
30688452 10.1021/acs.jmedchem.8b01465 Cytosolic carboxypeptidase 6 1
30688452 10.1021/acs.jmedchem.8b01465 Matrix metalloproteinase-9 1
30688452 10.1021/acs.jmedchem.8b01465 Stromelysin-2 1
30688452 10.1021/acs.jmedchem.8b01465 Macrophage metalloelastase 1
30688452 10.1021/acs.jmedchem.8b01465 Collagenase 3 1
30688452 10.1021/acs.jmedchem.8b01465 Papain 1
30688452 10.1021/acs.jmedchem.8b01465 Neutrophil elastase 1
30688452 10.1021/acs.jmedchem.8b01465 ADMET 1
30688452 10.1021/acs.jmedchem.8b01465 Carboxypeptidase B 1
30688452 10.1021/acs.jmedchem.8b01465 Carboxypeptidase D 1
30688452 10.1021/acs.jmedchem.8b01465 HeLa 1
30688452 10.1021/acs.jmedchem.8b01465 HEK-293T 1
30688452 10.1021/acs.jmedchem.8b01465 Carboxypeptidase A4 1

Data from ChEMBL 36 via Core Engine