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Compound Detail

CHEMBL4542919

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C#CC(=O)N(c1ccc(OC)cc1OC)C(C(=O)NCC(=O)OCC)c1cccs1

Basic Information

ChEMBL ID CHEMBL4542919
Phase Preclinical
Structure Type MOL
InChI Key AHOOZADJPNUFOQ-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

430.5
MW (Da)
2.15
ALogP
7
HBA
1
HBD
94.2
PSA (Ų)
0.48
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H22N2O6S
MW 430.48
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -1.34

Activity Summary

IC50 2 meas. best 5.0
EC50 1 meas. best 6.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Huh-7
CHEMBL614039
EC50 6.3 6.3 500.0 1
Protein disulfide-isomerase
CHEMBL5422
IC50 5.0 4.985 10000.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30759340 10.1021/acs.jmedchem.8b01951 U-87 MG 4
30759340 10.1021/acs.jmedchem.8b01951 Protein disulfide-isomerase 4
32830969 10.1021/acs.jmedchem.0c00728 Protein disulfide-isomerase 4
30759340 10.1021/acs.jmedchem.8b01951 A 172 3
30759340 10.1021/acs.jmedchem.8b01951 Eukaryotic translation initiation factor 2 subunit 1 2
30759340 10.1021/acs.jmedchem.8b01951 72 kDa type IV collagenase 1
30759340 10.1021/acs.jmedchem.8b01951 D54 cell line 1
38381886 10.1021/acs.jmedchem.3c02107 Protein disulfide-isomerase 1

Data from ChEMBL 36 via Core Engine