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Compound Detail

CHEMBL176161

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CN[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@H](CCCCN)C(=O)c1nc2ccccc2s1

Basic Information

ChEMBL ID CHEMBL176161
Phase Preclinical
Structure Type BOTH
InChI Key FDMCANZBBDCMIJ-ZLNRFVROSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

521.7
MW (Da)
2.91
ALogP
7
HBA
3
HBD
117.4
PSA (Ų)
0.25
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H35N5O3S
MW 521.69
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -0.52

Activity Summary

Ki 2 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine protease 1
CHEMBL3769
Ki 7.7 7.7 20.0 1
Prothrombin
CHEMBL204
Ki 6.68 6.68 210.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine protease 1 Ki = 20.0 nM 7.7 Binding affinity against bovine trypsin 15771442
Prothrombin Ki = 210.0 nM 6.68 Binding affinity determined against human alpha thrombin 15771442

Literature References

PubMed DOI Target Context # Activities
15771442 10.1021/jm0303857 Prothrombin 2
15771442 10.1021/jm0303857 Serine protease 1 1
15771442 10.1021/jm0303857 Homo sapiens 1
15771442 10.1021/jm0303857 Oryctolagus cuniculus 1

Data from ChEMBL 36 via Core Engine