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Compound Detail

CHEMBL1834418

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NCCCC[C@H](N)C(=O)Nc1ccc(Oc2ccc(S(=O)(=O)CC3CS3)cc2)cc1

Basic Information

ChEMBL ID CHEMBL1834418
Phase Preclinical
Structure Type MOL
InChI Key DJLYTRGAMWVKBZ-IJHRGXPZSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

449.6
MW (Da)
2.76
ALogP
7
HBA
3
HBD
124.5
PSA (Ų)
0.36
QED
0
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H27N3O4S2
MW 449.60
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -0.50

Activity Summary

Ki 2 meas. best 7.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
72 kDa type IV collagenase
CHEMBL333
Ki 7.21 7.21 62.0 1
Matrix metalloproteinase-9
CHEMBL321
Ki 5.8 5.8 1600.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.255 hr Homo sapiens
T1/2 0.4183 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21866961 10.1021/jm200566e Blood 2
21866961 10.1021/jm200566e No relevant target 2
21866961 10.1021/jm200566e Matrix metalloproteinase-9 1
21866961 10.1021/jm200566e 72 kDa type IV collagenase 1
21866961 10.1021/jm200566e Plasma 1

Data from ChEMBL 36 via Core Engine