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Compound Detail

CHEMBL254718

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CS(=O)(=O)N(C[C@@H](C(=O)NO)N1CCN(c2ccc(Cl)cc2)CC1)c1ccc(Oc2ccc(C(F)(F)F)cc2)cc1

Basic Information

ChEMBL ID CHEMBL254718
Phase Preclinical
Structure Type MOL
InChI Key GGFOVHADCXFYBC-VWLOTQADSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

613.1
MW (Da)
4.61
ALogP
7
HBA
2
HBD
102.4
PSA (Ų)
0.27
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H28ClF3N4O5S
MW 613.06
Aromatic Rings 3
Heavy Atoms 41
NP-Likeness -1.42

Activity Summary

IC50 2 meas. best 6.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
IC50 6.92 6.92 119.0 1
Matrix metalloproteinase-9
CHEMBL321
IC50 6.59 6.59 256.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
72 kDa type IV collagenase IC50 = 119.0 nM 6.92 Inhibition of MMP2 18083558
Matrix metalloproteinase-9 IC50 = 256.0 nM 6.59 Inhibition of MMP9 18083558

Literature References

PubMed DOI Target Context # Activities
18083558 10.1016/j.bmcl.2007.11.129 72 kDa type IV collagenase 1
18083558 10.1016/j.bmcl.2007.11.129 Matrix metalloproteinase-9 1
18083558 10.1016/j.bmcl.2007.11.129 Unchecked 1

Data from ChEMBL 36 via Core Engine