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Compound Detail

CHEMBL206963

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N=C(N)c1cc(CNC(=O)[C@@H]2C=CCN2C(=O)[C@@H](CC2CCCCC2)NCC(=O)O)sc1N

Basic Information

ChEMBL ID CHEMBL206963
Phase Preclinical
Structure Type MOL
InChI Key NRQVMRVMPKGSPS-SJORKVTESA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

476.6
MW (Da)
1.01
ALogP
7
HBA
6
HBD
174.6
PSA (Ų)
0.17
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H32N6O4S
MW 476.60
Aromatic Rings 1
Heavy Atoms 33
NP-Likeness -0.27

Activity Summary

IC50 1 meas. best 7.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
IC50 7.24 7.24 57.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin IC50 = 57.4 nM 7.24 Inhibition of thrombin 16517159

Literature References

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

Data from ChEMBL 36 via Core Engine