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Compound Detail

CHEMBL5184549

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CS(=O)(=O)Nc1ccc(Oc2ccc(S(=O)(=O)CC3CO3)cc2)cc1

Basic Information

ChEMBL ID CHEMBL5184549
Phase Preclinical
Structure Type MOL
InChI Key ADEXXMLIERNFQB-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

383.4
MW (Da)
2.02
ALogP
6
HBA
1
HBD
102.1
PSA (Ų)
0.73
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H17NO6S2
MW 383.45
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -0.99

Activity Summary

Ki 3 meas. best 5.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
Ki 5.62 5.62 2400.0 1
Interstitial collagenase
CHEMBL332
Ki 4.35 4.35 45000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
72 kDa type IV collagenase Ki = 2400.0 nM 5.62 Inhibition of MMP-2 (unknown origin) 35969157
Interstitial collagenase Ki = 45000.0 nM 4.35 Inhibition of MMP-1 (unknown origin) 35969157

Literature References

PubMed DOI Target Context # Activities
35969157 10.1021/acs.jmedchem.1c01855 Interstitial collagenase 1
35969157 10.1021/acs.jmedchem.1c01855 72 kDa type IV collagenase 1
35969157 10.1021/acs.jmedchem.1c01855 Stromelysin-1 1
35969157 10.1021/acs.jmedchem.1c01855 Matrilysin 1
35969157 10.1021/acs.jmedchem.1c01855 Matrix metalloproteinase-9 1
35969157 10.1021/acs.jmedchem.1c01855 Matrix metalloproteinase-14 1

Data from ChEMBL 36 via Core Engine