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Compound Detail

CHEMBL344421

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COc1cccc(-c2ccc3c(c2)C[C@@H]2OC(=O)C(C)(CCCCC(=N)N)[C@@H]32)c1

Basic Information

ChEMBL ID CHEMBL344421
Phase Preclinical
Structure Type MOL
InChI Key IHKFYTGOIRWQFJ-RJHJHSSFSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

392.5
MW (Da)
4.43
ALogP
4
HBA
2
HBD
85.4
PSA (Ų)
0.32
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H28N2O3
MW 392.50
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness 0.89

Activity Summary

IC50 1 meas. best 5.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
IC50 5.75 5.75 1800.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.67 hr -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin IC50 = 1800.0 nM 5.75 Inhibitory activity against human thrombin was determined 10091697

Literature References

PubMed DOI Target Context # Activities
10091697 10.1016/s0960-894x(99)00002-5 Prothrombin 1
10091697 10.1016/s0960-894x(99)00002-5 Serine protease 1 1
10091697 10.1016/s0960-894x(99)00002-5 NON-PROTEIN TARGET 1
10091697 10.1016/s0960-894x(99)00002-5 ADMET 1

Data from ChEMBL 36 via Core Engine