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Compound Detail

CHEMBL418923

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CCC(CC)N[C@@H](CC(=O)O)C(=O)N1CCCC[C@H]1CCOC1CCN(C(=N)N)CC1

Basic Information

ChEMBL ID CHEMBL418923
Phase Preclinical
Structure Type MOL
InChI Key BIUVZUVHMAGFKE-HKUYNNGSSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

439.6
MW (Da)
1.75
ALogP
5
HBA
4
HBD
132.0
PSA (Ų)
0.28
QED
0
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H41N5O4
MW 439.60
Aromatic Rings 0
Heavy Atoms 31
NP-Likeness -0.14

Activity Summary

Ki 2 meas. best 8.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 8.01 8.01 9.8 1
Serine protease 1
CHEMBL209
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 = 9.8 nM 8.01 In vitro inhibition of human thrombin. 12036353
Serine protease 1 Ki = 1400.0 nM 5.85 In vitro inhibition of human trypsin. 12036353

Literature References

PubMed DOI Target Context # Activities
12036353 10.1021/jm011133d Prothrombin 1
12036353 10.1021/jm011133d Serine protease 1 1
12036353 10.1021/jm011133d Thrombin & trypsin 1

Data from ChEMBL 36 via Core Engine