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Compound Detail

CHEMBL367237

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

Basic Information

ChEMBL ID CHEMBL367237
Phase Preclinical
Structure Type BOTH
InChI Key QIVIRMCXSHIRPU-BXOOBUKZSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

563.7
MW (Da)
2.23
ALogP
7
HBA
4
HBD
155.8
PSA (Ų)
0.11
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 C29H37N7O3S
MW 563.73
Aromatic Rings 3
Heavy Atoms 40
NP-Likeness -0.42

Activity Summary

IC50 1 meas. best 5.43
Ki 1 meas. best 5.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
IC50 5.43 5.43 3700.0 1
Serine protease 1
CHEMBL3769
Ki 5.22 5.22 6000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin IC50 = 3700.0 nM 5.43 Inhibitory concentration against human alpha thrombin 15771442
Serine protease 1 Ki = 6000.0 nM 5.22 Binding affinity against bovine trypsin 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