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Compound Detail

CHEMBL4085013

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CC(NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)CCCC[C@@H]1SC[C@@H]2NC(=O)N[C@@H]21)P(=O)(Oc1ccc(Cl)cc1)Oc1ccc(Cl)cc1

Basic Information

ChEMBL ID CHEMBL4085013
Phase Preclinical
Structure Type MOL
InChI Key LZSHSERVJMFGOL-NQFWNBCBSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

947.8
MW (Da)
5.22
ALogP
11
HBA
7
HBD
241.8
PSA (Ų)
0.04
QED
4
Ro5 Violations
20
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C42H49Cl2N6O11PS
MW 947.83
Aromatic Rings 3
Heavy Atoms 63
NP-Likeness -0.24

Activity Summary

Ki 1 meas. best 7.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Myeloblastin
CHEMBL3900
Ki 7.68 7.68 21.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Myeloblastin Ki = 21.0 nM 7.68 Inhibition of human PR3 using ABZ-VADnVADYQ-EDDnp as substrate by FRET assay 29442501

Literature References

PubMed DOI Target Context # Activities
29442501 10.1021/acs.jmedchem.7b01416 Myeloblastin 3
29442501 10.1021/acs.jmedchem.7b01416 Unchecked 1
29442501 10.1021/acs.jmedchem.7b01416 Neutrophil elastase 1

Data from ChEMBL 36 via Core Engine