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Compound Detail

CHEMBL199917

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O=C(Nc1ccc(S(=O)(=O)C[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)cc1)c1ccc(Br)cc1

Basic Information

ChEMBL ID CHEMBL199917
Phase Preclinical
Structure Type MOL
InChI Key GJITXIQQHBXCIH-GOSISDBHSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

541.4
MW (Da)
4.90
ALogP
4
HBA
3
HBD
116.3
PSA (Ų)
0.29
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H21BrN2O5S
MW 541.42
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.02

Activity Summary

IC50 2 meas. best 8.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
IC50 8.59 8.59 2.6 1
Matrix metalloproteinase-9
CHEMBL321
IC50 8.57 8.57 2.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
72 kDa type IV collagenase IC50 = 2.6 nM 8.59 Binding affinity to MMP2 16392792
Matrix metalloproteinase-9 IC50 = 2.7 nM 8.57 Binding affinity to MMP9 16392792

Literature References

PubMed DOI Target Context # Activities
16392792 10.1021/jm050363f Interstitial collagenase 1
16392792 10.1021/jm050363f Stromelysin-1 1
16392792 10.1021/jm050363f 72 kDa type IV collagenase 1
16392792 10.1021/jm050363f Matrix metalloproteinase-9 1
16392792 10.1021/jm050363f Matrilysin 1

Data from ChEMBL 36 via Core Engine