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Compound Detail

CHEMBL402378

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N=C(N)N1CCC[C@@H](C[C@H](NC(=O)CN2C(=O)CN(CCCc3ccccc3)C(=O)[C@H]2Cc2ccccc2Cl)C(=O)c2nccs2)C1

Basic Information

ChEMBL ID CHEMBL402378
Phase Preclinical
Structure Type MOL
InChI Key CTVGDUDNNKYLJB-SAAIGDAKSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

678.3
MW (Da)
3.37
ALogP
7
HBA
3
HBD
152.8
PSA (Ų)
0.14
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 C34H40ClN7O4S
MW 678.26
Aromatic Rings 3
Heavy Atoms 47
NP-Likeness -0.79

Activity Summary

IC50 1 meas. best 5.01
Ki 1 meas. best 8.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 8.92 8.92 1.2 1
Trypsin
CHEMBL2095204
IC50 5.01 5.01 9700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 1.2 nM 8.92 Inhibition of human alpha-thrombin 18053726
Trypsin IC50 = 9700.0 nM 5.01 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
18053726 10.1016/j.bmc.2007.11.015 Unchecked 1

Data from ChEMBL 36 via Core Engine