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Compound Detail

CHEMBL4099333

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CC(=O)N[C@H]1CSCc2cc3cc(c2)CSC[C@H](NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C2CCN2C(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CO)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)O)CSC3

Basic Information

ChEMBL ID CHEMBL4099333
Phase Preclinical
Structure Type MOL
InChI Key BZKNNTULLXYXIY-PMRUMLPOSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

1688.0
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C75H106N20O19S3
MW 1688.00

Activity Summary

Ki 1 meas. best 9.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasma kallikrein
CHEMBL2000
Ki 9.85 9.85 0.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Plasma kallikrein Ki = 0.14 nM 9.85 Inhibition of human plasma kallikrein using fluorogenic H-Pro-Phe-Arg-AMC peptid... 29517911

Literature References

PubMed DOI Target Context # Activities
29517911 10.1021/acs.jmedchem.7b01625 Plasma kallikrein 1

Data from ChEMBL 36 via Core Engine