Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL4059991

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
CC(=O)N[C@H]1CSCc2cc3cc(c2)CSC[C@H](C(=O)N[C@@H](C)C(=O)N(C)CC(=O)N(C)CC(=O)N(C)CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](CCCNC(=N)N)C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CSC3)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(N)=O)NC1=O

Basic Information

ChEMBL ID CHEMBL4059991
Phase Preclinical
Structure Type MOL
InChI Key OHOYFNPMBCNOTR-QFZQKJJLSA-N
7
Targets
11
Activities
2
Assay Types
6
PK Parameters
20
Publications
0
Known Names

Molecular Properties

2559.0
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C117H160N32O28S3
MW 2558.96

Activity Summary

Ki 9 meas. best 8.52
IC50 2 meas. best 7.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasma kallikrein
CHEMBL2000
Ki 8.52 8.52 3.0 1
Unchecked
CHEMBL612545
Ki 8.51 6.8833 3.1 3
Plasma kallikrein
CHEMBL4105792
Ki 8.47 8.47 3.4 1
Plasma kallikrein
CHEMBL2000
IC50 7.57 6.835 27.0 2
Plasma kallikrein
CHEMBL1250359
Ki 7.27 7.27 54.0 1
Kallikrein 1
CHEMBL4064
Ki 6.39 6.39 410.0 1
Suppressor of tumorigenicity 14 protein
CHEMBL3018
Ki 4.4 4.4 40000.0 1
Kallikrein-5
CHEMBL4447
Ki 4.3 4.3 50000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 8.2 mL.min-1.kg-1 Rattus norvegicus
T1/2 24.0 hr Homo sapiens
T1/2 24.0 hr Rattus norvegicus
T1/2 24.0 hr Mus musculus
T1/2 24.0 hr Homo sapiens
T1/2 1.3 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

Data from ChEMBL 36 via Core Engine