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Compound Detail

CHEMBL206418

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N=C(N)c1ccc(CNC(=O)[C@@H]2C=CCN2C(=O)[C@@H](CC2CCCCC2)NCC(=O)O)cc1

Basic Information

ChEMBL ID CHEMBL206418
Phase Preclinical
Structure Type MOL
InChI Key KVGJPCGVLIPRKV-UXHICEINSA-N
1
Targets
2
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

455.6
MW (Da)
1.37
ALogP
5
HBA
5
HBD
148.6
PSA (Ų)
0.20
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H33N5O4
MW 455.56
Aromatic Rings 1
Heavy Atoms 33
NP-Likeness -0.10

Activity Summary

IC50 2 meas. best 8.78

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
IC50 8.78 8.775 1.7 2

Pharmacokinetic Data

Parameter Value Units Species
AUC 168.0 s Canis lupus familiaris
F 35.0 % Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin IC50 = 1.68 nM 8.78 Inhibition of thrombin 16517159
Prothrombin IC50 = 1.7 nM 8.77 Inhibition of thrombin by chromogenic assay 16460939

Literature References

PubMed DOI Target Context # Activities
16517159 10.1016/j.bmcl.2006.02.040 Rattus norvegicus 2
16460939 10.1016/j.bmcl.2006.01.046 Canis familiaris 2
16517159 10.1016/j.bmcl.2006.02.040 Prothrombin 1
16460939 10.1016/j.bmcl.2006.01.046 Prothrombin 1

Data from ChEMBL 36 via Core Engine