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Compound Detail

CHEMBL179245

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CN[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)NC(CCCN=C(N)N)C(=O)c1nc2ccc(C(N)=O)cc2s1

Basic Information

ChEMBL ID CHEMBL179245
Phase Preclinical
Structure Type MOL
InChI Key BRWGCIHUFVUAFZ-PDQYLBCOSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

592.7
MW (Da)
0.94
ALogP
8
HBA
5
HBD
198.9
PSA (Ų)
0.08
QED
1
Ro5 Violations
13
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 -0.47

Activity Summary

IC50 1 meas. best 8.3
Ki 1 meas. best 9.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine protease 1
CHEMBL3769
Ki 9.52 9.52 0.3 1
Prothrombin
CHEMBL204
IC50 8.3 8.3 5.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine protease 1 Ki = 0.3 nM 9.52 Binding affinity against bovine trypsin 15771442
Prothrombin IC50 = 5.0 nM 8.3 Inhibitory concentration 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

Data from ChEMBL 36 via Core Engine