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Compound Detail

CHEMBL4169884

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C#CC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@@H]3CSSC[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)[C@H](Cc4c[nH]c5ccc(Br)cc45)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCC)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC1=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N3)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC2=O

Basic Information

ChEMBL ID CHEMBL4169884
Phase Preclinical
Structure Type MOL
InChI Key VEEQSZWXUOUXPZ-ZEGFWLDJSA-N
5
Targets
5
Activities
1
Assay Types
5
PK Parameters
7
Publications
0
Known Names

Molecular Properties

3777.3
MW (Da)

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C162H245BrN48O40S6
MW 3777.34

Activity Summary

IC50 5 meas. best 9.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium channel protein type 9 subunit alpha
CHEMBL4296
IC50 9.59 9.59 0.3 1
Sodium channel protein type 4 subunit alpha
CHEMBL2072
IC50 7.28 7.28 53.0 1
Sodium channel protein type 8 subunit alpha
CHEMBL5202
IC50 7.18 7.18 66.0 1
Sodium channel protein type 5 subunit alpha
CHEMBL1980
IC50 6.58 6.58 260.0 1
Sodium channel protein type 10 subunit alpha
CHEMBL5451
IC50 6.29 6.29 509.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 12994.05 ng.hr.mL-1 Mus musculus
Cmax 892.0 nM Mus musculus
MRT 3.55 hr Mus musculus
T1/2 2.38 hr Mus musculus
Tmax 0.5 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30346167 10.1021/acs.jmedchem.8b00736 Mus musculus 7
30346167 10.1021/acs.jmedchem.8b00736 Sodium channel protein type 9 subunit alpha 1
30346167 10.1021/acs.jmedchem.8b00736 Sodium channel protein type 4 subunit alpha 1
30346167 10.1021/acs.jmedchem.8b00736 Sodium channel protein type 8 subunit alpha 1
30346167 10.1021/acs.jmedchem.8b00736 Sodium channel protein type 5 subunit alpha 1
30346167 10.1021/acs.jmedchem.8b00736 Sodium channel protein type 10 subunit alpha 1
30346167 10.1021/acs.jmedchem.8b00736 ADMET 1

Data from ChEMBL 36 via Core Engine