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Compound Detail

CHEMBL3780208

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N=C(N)c1cccc(N2CC(OCc3ccccc3)CN(CC3CCN(Cc4ccccc4)CC3)C2=O)c1

Basic Information

ChEMBL ID CHEMBL3780208
Phase Preclinical
Structure Type MOL
InChI Key MEELSFYQUGSNNK-UHFFFAOYSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

511.7
MW (Da)
4.71
ALogP
4
HBA
2
HBD
85.9
PSA (Ų)
0.32
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H37N5O2
MW 511.67
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -1.02

Activity Summary

Ki 6 meas. best 6.26

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypsin
CHEMBL2095204
Ki 6.26 6.26 550.0 1
Serine protease hepsin
CHEMBL2079849
Ki 6.12 6.12 760.0 1
Coagulation factor X
CHEMBL244
Ki 6.04 6.04 920.0 1
Suppressor of tumorigenicity 14 protein
CHEMBL3018
Ki 5.81 5.81 1540.0 1
Hepatocyte growth factor activator
CHEMBL3351190
Ki 5.72 5.72 1920.0 1
Prothrombin
CHEMBL204
Ki 4.53 4.53 29700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26985294 10.1021/acsmedchemlett.5b00357 No relevant target 2
26985294 10.1021/acsmedchemlett.5b00357 Suppressor of tumorigenicity 14 protein 1
26985294 10.1021/acsmedchemlett.5b00357 Serine protease hepsin 1
26985294 10.1021/acsmedchemlett.5b00357 Hepatocyte growth factor activator 1
26985294 10.1021/acsmedchemlett.5b00357 Trypsin 1
26985294 10.1021/acsmedchemlett.5b00357 Prothrombin 1
26985294 10.1021/acsmedchemlett.5b00357 Coagulation factor X 1

Data from ChEMBL 36 via Core Engine