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Compound Detail

CHEMBL209334

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N=C(N)NCCC(=O)N1CCN(C(=O)[C@H](Cc2cccc(C(=N)N)c2)NS(=O)(=O)Cc2ccc3ccccc3c2)CC1

Basic Information

ChEMBL ID CHEMBL209334
Phase Preclinical
Structure Type MOL
InChI Key SZACOCRLRDPNPP-VWLOTQADSA-N
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

592.7
MW (Da)
0.70
ALogP
6
HBA
6
HBD
198.6
PSA (Ų)
0.14
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H36N8O4S
MW 592.73
Aromatic Rings 3
Heavy Atoms 42
NP-Likeness -0.90

Activity Summary

Ki 5 meas. best 6.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Suppressor of tumorigenicity 14 protein
CHEMBL3018
Ki 6.4 6.4 400.0 1
Prothrombin
CHEMBL204
Ki 5.58 5.58 2600.0 1
Plasminogen
CHEMBL1801
Ki 4.92 4.92 12000.0 1
Urokinase-type plasminogen activator
CHEMBL3286
Ki 4.37 4.37 43000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Suppressor of tumorigenicity 14 protein Ki = 400.0 nM 6.4 Inhibition of matriptase 16821772
Prothrombin Ki = 2600.0 nM 5.58 Inhibition of thrombin 16821772
Plasminogen Ki = 12000.0 nM 4.92 Inhibition of plasmin 16821772
Urokinase-type plasminogen activator Ki = 43000.0 nM 4.37 Inhibition of uPA 16821772

Literature References

PubMed DOI Target Context # Activities
16821772 10.1021/jm051272l Coagulation factor X 1
16821772 10.1021/jm051272l Prothrombin 1
16821772 10.1021/jm051272l Plasminogen 1
16821772 10.1021/jm051272l Urokinase-type plasminogen activator 1
16821772 10.1021/jm051272l Suppressor of tumorigenicity 14 protein 1

Data from ChEMBL 36 via Core Engine