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Compound Detail

CHEMBL73928

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O=CN(O)C(CS(=O)(=O)c1ccc(Oc2ccc(OC(F)(F)F)cc2)cc1)c1ccccn1

Basic Information

ChEMBL ID CHEMBL73928
Phase Preclinical
Structure Type MOL
InChI Key YHQIGEQPWJUUHA-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

482.4
MW (Da)
4.14
ALogP
7
HBA
1
HBD
106.0
PSA (Ų)
0.28
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H17F3N2O6S
MW 482.44
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.11

Activity Summary

IC50 3 meas. best 8.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
IC50 8.77 8.77 1.7 1
Matrix metalloproteinase-9
CHEMBL321
IC50 8.66 8.66 2.2 2

Pharmacokinetic Data

Parameter Value Units Species
AUC 482.44 ng.hr.mL-1 Simiiformes

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11754593 10.1021/jm0103920 Interstitial collagenase 1
11754593 10.1021/jm0103920 72 kDa type IV collagenase 1
11754593 10.1021/jm0103920 Matrix metalloproteinase-9 1
11754593 10.1021/jm0103920 ADMET 1
24900330 10.1021/ml200031m Matrix metalloproteinase-9 1

Data from ChEMBL 36 via Core Engine