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Compound Detail

CHEMBL52107

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CNC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CC(=O)NNS(=O)(=O)c1ccc(C)cc1)CC(C)C

Basic Information

ChEMBL ID CHEMBL52107
Phase Preclinical
Structure Type MOL
InChI Key OUDOQEURKMFZDS-PHSANKKPSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

541.7
MW (Da)
2.31
ALogP
5
HBA
5
HBD
149.3
PSA (Ų)
0.22
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H35N5O5S
MW 541.67
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -0.75

Activity Summary

IC50 1 meas. best 7.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
IC50 7.52 7.52 30.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
72 kDa type IV collagenase IC50 = 30.0 nM 7.52 Inhibition of Matrix metalloprotease-2 12729664

Literature References

PubMed DOI Target Context # Activities
12729664 10.1016/s0960-894x(03)00214-2 Interstitial collagenase 1
12729664 10.1016/s0960-894x(03)00214-2 72 kDa type IV collagenase 1

Data from ChEMBL 36 via Core Engine