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Compound Detail

CHEMBL101855

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CN[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)c1nc2ccccc2[nH]1

Basic Information

ChEMBL ID CHEMBL101855
Phase Preclinical
Structure Type BOTH
InChI Key DPKBODMBRLVNFI-ZRBLBEILSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

532.6
MW (Da)
1.11
ALogP
6
HBA
5
HBD
171.6
PSA (Ų)
0.10
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 C28H36N8O3
MW 532.65
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness -0.08

Activity Summary

Ki 3 meas. best 8.02

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 8.02 7.97 9.6 2
Serine protease 1
CHEMBL3769
Ki 7.42 7.42 38.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 9.6 nM 8.02 Binding affinity to human thrombin 14761180
Prothrombin Ki = 12.0 nM 7.92 Inhibition of human alpha-thrombin. 8759623
Serine protease 1 Ki = 38.0 nM 7.42 Inhibition of bovine trypsin 8759623

Literature References

PubMed DOI Target Context # Activities
14761180 10.1021/jm030493t Prothrombin 1
14761180 10.1021/jm030493t Thrombin & trypsin 1
8759623 10.1021/jm9603274 Prothrombin 1
8759623 10.1021/jm9603274 Serine protease 1 1
8759623 10.1021/jm9603274 Unchecked 1

Data from ChEMBL 36 via Core Engine