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Compound Detail

CHEMBL4085021

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N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1cscn1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)c1nc2ccccc2s1

Basic Information

ChEMBL ID CHEMBL4085021
Phase Preclinical
Structure Type MOL
InChI Key WHTKMCKEGVQWOA-SYKYGTKKSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

771.9
MW (Da)
2.12
ALogP
12
HBA
9
HBD
258.5
PSA (Ų)
0.03
QED
3
Ro5 Violations
18
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C37H41N9O6S2
MW 771.93
Aromatic Rings 5
Heavy Atoms 54
NP-Likeness -0.39

Activity Summary

Ki 2 meas. best 7.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Transmembrane protease serine 6
CHEMBL1795139
Ki 7.89 7.89 13.0 1
Suppressor of tumorigenicity 14 protein
CHEMBL3018
Ki 7.7 7.7 20.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28219045 10.1016/j.ejmech.2017.02.006 Transmembrane protease serine 6 1
28219045 10.1016/j.ejmech.2017.02.006 Suppressor of tumorigenicity 14 protein 1
28219045 10.1016/j.ejmech.2017.02.006 Unchecked 1

Data from ChEMBL 36 via Core Engine