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Compound Detail

CHEMBL3417770

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CNC(=O)c1ccc(Oc2ccc(S(=O)(=O)[C@]3(C(=O)NO)CCC4(CCNCC4)C3)cc2)cc1

Basic Information

ChEMBL ID CHEMBL3417770
Phase Preclinical
Structure Type MOL
InChI Key ZUZGJCNWNOCKEB-XMMPIXPASA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
14
Publications
0
Known Names

Molecular Properties

487.6
MW (Da)
2.41
ALogP
7
HBA
4
HBD
133.8
PSA (Ų)
0.36
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H29N3O6S
MW 487.58
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -0.31

Activity Summary

IC50 2 meas. best 7.92
EC50 1 meas. best 9.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Blood
CHEMBL613416
EC50 9.15 9.15 0.7 1
Stromelysin-2
CHEMBL4270
IC50 7.92 7.92 12.0 1
Stromelysin-1
CHEMBL283
IC50 7.82 7.82 15.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25686153 10.1021/jm501940y Liver microsome 2
25686153 10.1021/jm501940y Voltage-gated inwardly rectifying potassium channel KCNH2 2
25686153 10.1021/jm501940y ADMET 2
25686153 10.1021/jm501940y Blood 1
25686153 10.1021/jm501940y Stromelysin-2 1
25686153 10.1021/jm501940y Stromelysin-1 1
25686153 10.1021/jm501940y Cytochrome P450 1A2 1
25686153 10.1021/jm501940y Cytochrome P450 2C9 1
25686153 10.1021/jm501940y Cytochrome P450 2C19 1
25686153 10.1021/jm501940y Cytochrome P450 2D6 1
25686153 10.1021/jm501940y Cytochrome P450 3A4 1
25686153 10.1021/jm501940y Liver 1
25686153 10.1021/jm501940y Mus musculus 1
25686153 10.1021/jm501940y No relevant target 1

Data from ChEMBL 36 via Core Engine