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Compound Detail

CHEMBL4588728

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CSCC[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@@H](N)CC(=O)O)CSSC[C@@H]2NC(=O)[C@@H]3CSSC[C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](Cc4c[nH]c5ccccc45)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc4ccccc4)C(=O)N[C@H](C(=O)N[C@@H](Cc4ccccc4)C(=O)N[C@H](C(=O)O)[C@@H](C)O)[C@@H](C)O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@H](Cc4ccccc4)NC1=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N3)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCCN)NC2=O

Basic Information

ChEMBL ID CHEMBL4588728
Phase Preclinical
Structure Type MOL
InChI Key DFBDAHMZXJYZJG-AALCJKKVSA-N
10
Targets
10
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

4272.0
MW (Da)

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C183H265N49O54S8
MW 4271.96

Activity Summary

IC50 10 meas. best 9.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium channel protein type 7 subunit alpha
CHEMBL3585
IC50 9.05 9.05 0.9 1
Sodium channel protein type 9 subunit alpha
CHEMBL3312
IC50 8.82 8.82 1.5 1
Sodium channel protein type 9 subunit alpha
CHEMBL3414411
IC50 8.36 8.36 4.4 1
Sodium channel protein type 1 subunit alpha
CHEMBL1845
IC50 7.43 7.43 37.0 1
Sodium channel protein type 2 subunit alpha
CHEMBL4187
IC50 6.92 6.92 120.0 1
Sodium channel protein type 8 subunit alpha
CHEMBL5202
IC50 6.89 6.89 130.0 1
Sodium channel protein type 4 subunit alpha
CHEMBL2072
IC50 6.85 6.85 140.0 1
Sodium channel protein type 3 subunit alpha
CHEMBL5163
IC50 6.68 6.68 210.0 1
Sodium channel protein type 5 subunit alpha
CHEMBL1980
IC50 6.1 6.1 800.0 1
Sodium channel protein type 10 subunit alpha
CHEMBL5451
IC50 4.3 4.3 50000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sodium channel protein type 7 subunit alpha IC50 = 0.9 nM 9.05 Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay 31012583
Sodium channel protein type 9 subunit alpha IC50 = 1.5 nM 8.82 Inhibition of rat Nav1.7 expressed in HEK293 cells by electrophysiology assay 31012583
Sodium channel protein type 9 subunit alpha IC50 = 4.4 nM 8.36 Inhibition of mouse Nav1.7 expressed in HEK293 cells by electrophysiology assay 31012583
Sodium channel protein type 1 subunit alpha IC50 = 37.0 nM 7.43 Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay 31012583
Sodium channel protein type 2 subunit alpha IC50 = 120.0 nM 6.92 Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay 31012583
Sodium channel protein type 8 subunit alpha IC50 = 130.0 nM 6.89 Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay 31012583
Sodium channel protein type 4 subunit alpha IC50 = 140.0 nM 6.85 Inhibition of human Nav1.4 expressed in HEK293 cells by electrophysiology assay 31012583
Sodium channel protein type 3 subunit alpha IC50 = 210.0 nM 6.68 Inhibition of human Nav1.3 expressed in HEK293 cells by electrophysiology assay 31012583
Sodium channel protein type 5 subunit alpha IC50 = 800.0 nM 6.1 Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay 31012583
Sodium channel protein type 10 subunit alpha IC50 = 50000.0 nM 4.3 Inhibition of human Nav1.8 expressed in HEK293 cells by electrophysiology assay 31012583

Literature References

PubMed DOI Target Context # Activities
31012583 10.1021/acs.jmedchem.8b01906 Unchecked 7
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 9 subunit alpha 2
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 7 subunit alpha 1
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 1 subunit alpha 1
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 2 subunit alpha 1
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 3 subunit alpha 1
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 4 subunit alpha 1
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 5 subunit alpha 1
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 8 subunit alpha 1
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 10 subunit alpha 1

Data from ChEMBL 36 via Core Engine