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Compound Detail

CHEMBL355060

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NCCCC[C@H](NC(=O)[C@@H]1CC[C@H]2CN(C(=O)CCc3ccccc3)CC(=O)N21)C(=O)c1nccs1

Basic Information

ChEMBL ID CHEMBL355060
Phase Preclinical
Structure Type MOL
InChI Key UCMGNZDFXFVZPC-ACRUOGEOSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

511.6
MW (Da)
1.77
ALogP
7
HBA
2
HBD
125.7
PSA (Ų)
0.35
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H33N5O4S
MW 511.65
Aromatic Rings 2
Heavy Atoms 36
NP-Likeness -0.58

Activity Summary

IC50 2 meas. best 7.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine protease 1
CHEMBL209
IC50 7.85 7.85 14.0 1
Prothrombin
CHEMBL204
IC50 7.11 7.11 77.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine protease 1 IC50 = 14.0 nM 7.85 In vitro inhibitory activity against human trypsin 10206546
Prothrombin IC50 = 77.0 nM 7.11 Inhibition of human Thrombin 10206546

Literature References

PubMed DOI Target Context # Activities
10206546 10.1016/s0960-894x(99)00096-7 Prothrombin 1
10206546 10.1016/s0960-894x(99)00096-7 Serine protease 1 1
10206546 10.1016/s0960-894x(99)00096-7 Thrombin & trypsin 1

Data from ChEMBL 36 via Core Engine