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Compound Detail

CHEMBL256394

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N=C(N)N1CCC[C@@H](C[C@H](NC(=O)CN2C(=O)CN(CCCc3ccccc3)C(=O)[C@@H]2Cc2ccccc2)C(=O)c2nccs2)C1

Basic Information

ChEMBL ID CHEMBL256394
Phase Preclinical
Structure Type MOL
InChI Key VLENRKZVWUVYFG-KCHLEUMXSA-N
1
Targets
3
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

643.8
MW (Da)
2.72
ALogP
7
HBA
3
HBD
152.8
PSA (Ų)
0.15
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 C34H41N7O4S
MW 643.81
Aromatic Rings 3
Heavy Atoms 46
NP-Likeness -0.59

Activity Summary

Ki 2 meas. best 7.62
IC50 1 meas. best 6.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 7.62 7.62 24.0 2
Prothrombin
CHEMBL204
IC50 6.62 6.62 240.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 24.0 nM 7.62 Binding affinity against thrombin 10498196
Prothrombin Ki = 24.0 nM 7.62 Inhibition of human alpha-thrombin 18053726
Prothrombin IC50 = 240.0 nM 6.62 Inhibitory activity against human thrombin 10498196

Literature References

PubMed DOI Target Context # Activities
10498196 10.1016/s0960-894x(99)00418-7 Prothrombin 2
10498196 10.1016/s0960-894x(99)00418-7 Serine protease 1 1
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