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Compound Detail

CHEMBL569445

GRASSYSTATIN C
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CC[C@H](C)[C@H](NC(=O)C[C@H](O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)N(C)C(=O)[C@H](CC(C)C)NC(=O)[C@H](O)[C@@H](C)CC)C(=O)NCC(=O)N(C)[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)OC

Basic Information

ChEMBL ID CHEMBL569445
Name GRASSYSTATIN C
Phase Preclinical
Structure Type MOL
InChI Key CRTPOZWNLFMWPB-YQGVOMCUSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

987.2
MW (Da)
1.18
ALogP
12
HBA
7
HBD
287.2
PSA (Ų)
0.06
QED
3
Ro5 Violations
29
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C50H82N8O12
MW 987.25
Aromatic Rings 1
Heavy Atoms 70
NP-Likeness 0.13

Activity Summary

IC50 3 meas. best 7.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin E
CHEMBL3092
IC50 7.37 7.37 42.9 1
Cathepsin D
CHEMBL2581
IC50 5.79 5.79 1620.0 1
Disintegrin and metalloproteinase domain-containing protein 17
CHEMBL3706
IC50 4.54 4.54 28600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin E IC50 = 42.9 nM 7.37 Inhibition of cathepsin E 19715320
Cathepsin D IC50 = 1620.0 nM 5.79 Inhibition of cathepsin D 19715320
Disintegrin and metalloproteinase domain-containing protein 17 IC50 = 28600.0 nM 4.54 Inhibition of TACE 19715320

Literature References

PubMed DOI Target Context # Activities
19715320 10.1021/jm9009394 Unchecked 1
19715320 10.1021/jm9009394 Cathepsin D 1
19715320 10.1021/jm9009394 Cathepsin E 1
19715320 10.1021/jm9009394 Disintegrin and metalloproteinase domain-containing protein 9 1
19715320 10.1021/jm9009394 Disintegrin and metalloproteinase domain-containing protein 10 1
19715320 10.1021/jm9009394 Disintegrin and metalloproteinase domain-containing protein 17 1

Data from ChEMBL 36 via Core Engine