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Compound Detail

CHEMBL4094620

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COc1cccc(-c2csc3nc(C(=O)NCc4cccc(OCCOc5nc[nH]n5)c4)[nH]c(=O)c23)c1

Basic Information

ChEMBL ID CHEMBL4094620
Phase Preclinical
Structure Type MOL
InChI Key UIAVJVYRIHXLAO-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

518.6
MW (Da)
3.17
ALogP
9
HBA
3
HBD
144.1
PSA (Ų)
0.24
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H22N6O5S
MW 518.56
Aromatic Rings 5
Heavy Atoms 37
NP-Likeness -1.56

Activity Summary

IC50 1 meas. best 10.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Collagenase 3
CHEMBL280
IC50 10.59 10.59 0.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 24.0 ng.hr.mL-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Collagenase 3 IC50 = 0.026 nM 10.59 Inhibition of APMA-activated recombinant human MMP-13 using Cy3-PLGLK(Cy5Q)AR-NH... 27966948

Literature References

PubMed DOI Target Context # Activities
27966948 10.1021/acs.jmedchem.6b01007 Collagenase 3 1
27966948 10.1021/acs.jmedchem.6b01007 Cytochrome P450 3A4 1
27966948 10.1021/acs.jmedchem.6b01007 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine