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Compound Detail

CHEMBL4159737

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CON(C)C(=O)C1(S(=O)(=O)c2ccc(Oc3ccc(OC(F)(F)F)cc3)cc2)CCC2(CCNCC2)C1

Basic Information

ChEMBL ID CHEMBL4159737
Phase Preclinical
Structure Type MOL
InChI Key YIVHYRNDAKHULZ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

542.6
MW (Da)
4.46
ALogP
7
HBA
1
HBD
94.2
PSA (Ų)
0.52
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H29F3N2O6S
MW 542.58
Aromatic Rings 2
Heavy Atoms 37
NP-Likeness -0.52

Activity Summary

EC50 1 meas. best 5.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Blood
CHEMBL613416
EC50 5.43 5.43 3700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Blood EC50 = 3700.0 nM 5.43 Antifibrinolytic activity in human whole blood assessed as concentration of comp... 29795754

Literature References

PubMed DOI Target Context # Activities
29795754 10.1021/acsmedchemlett.7b00549 Blood 1
29795754 10.1021/acsmedchemlett.7b00549 Stromelysin-1 1
29795754 10.1021/acsmedchemlett.7b00549 Stromelysin-2 1

Data from ChEMBL 36 via Core Engine