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Compound Detail

CHEMBL268833

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CS(=O)(=O)N[C@@H](C(=O)N1CCC[C@H]1C(=O)NCc1cc(CN)cs1)C(c1ccccc1)c1ccccc1

Basic Information

ChEMBL ID CHEMBL268833
Phase Preclinical
Structure Type MOL
InChI Key QCMOXWKNGSNGLJ-UKILVPOCSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

540.7
MW (Da)
2.56
ALogP
6
HBA
3
HBD
121.6
PSA (Ų)
0.36
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H32N4O4S2
MW 540.71
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -0.96

Activity Summary

Ki 2 meas. best 8.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 8.62 8.62 2.4 1
Serine protease 1
CHEMBL3769
Ki 7.17 7.17 68.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 2.4 nM 8.62 Binding affinity against human thrombin 11909707
Serine protease 1 Ki = 68.0 nM 7.17 Binding affinity against bovine trypsin 11909707

Literature References

PubMed DOI Target Context # Activities
11909707 10.1016/s0960-894x(02)00093-8 Prothrombin 1
11909707 10.1016/s0960-894x(02)00093-8 Serine protease 1 1
11909707 10.1016/s0960-894x(02)00093-8 Coagulation factor X 1
11909707 10.1016/s0960-894x(02)00093-8 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine