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Compound Detail

CHEMBL4126311

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CSCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@]1(C)CCC/C=C\CCC[C@@](C)(C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC1=O)C(C)C)C(C)C

Basic Information

ChEMBL ID CHEMBL4126311
Phase Preclinical
Structure Type MOL
InChI Key ZEXNMYVOVAJSAS-DHLBLOESSA-N
1
Targets
5
Activities
1
Assay Types
5
PK Parameters
5
Publications
0
Known Names

Molecular Properties

2591.1
MW (Da)

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C120H192N26O35S
MW 2591.07

Activity Summary

EC50 5 meas. best 6.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
EC50 6.48 6.016 330.0 5

Pharmacokinetic Data

Parameter Value Units Species
AUC 91300.0 ng.hr.mL-1 Rattus norvegicus
CL 0.6833 mL.min-1.kg-1 Rattus norvegicus
Cmax 38092.37 nM Rattus norvegicus
T1/2 1.15 hr Rattus norvegicus
Vd 0.066 L.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29442512 10.1021/acs.jmedchem.7b01732 Unchecked 10
29442512 10.1021/acs.jmedchem.7b01732 Rattus norvegicus 6
29442512 10.1021/acs.jmedchem.7b01732 Huh-7 1
29442512 10.1021/acs.jmedchem.7b01732 Calu-3 1
29442512 10.1021/acs.jmedchem.7b01732 No relevant target 1

Data from ChEMBL 36 via Core Engine