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Compound Detail

CHEMBL256631

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N[C@H]1CC[C@H]([C@H](NC(=O)[C@@H]2CC[C@H]3CN(S(=O)(=O)Cc4ccccc4)CC(=O)N32)C(=O)c2nc3ccccc3s2)CC1

Basic Information

ChEMBL ID CHEMBL256631
Phase Preclinical
Structure Type MOL
InChI Key CTKFXSVIDQTFTB-IOWQSWGASA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

609.8
MW (Da)
2.69
ALogP
8
HBA
2
HBD
142.8
PSA (Ų)
0.37
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H35N5O5S2
MW 609.77
Aromatic Rings 3
Heavy Atoms 42
NP-Likeness -1.16

Activity Summary

Ki 2 meas. best 9.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 9.15 9.15 0.7 1
Trypsin
CHEMBL2095204
Ki 5.85 5.85 1400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 0.7 nM 9.15 Inhibition of human alpha-thrombin 18053726
Trypsin Ki = 1400.0 nM 5.85 Inhibition of human trypsin 18053726

Literature References

PubMed DOI Target Context # Activities
18053726 10.1016/j.bmc.2007.11.015 Prothrombin 1
18053726 10.1016/j.bmc.2007.11.015 Trypsin 1

Data from ChEMBL 36 via Core Engine