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Compound Detail

CHEMBL1159685

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N=C(N)c1ccc(CNC(=O)[C@@H]2CCCN2C(=O)[C@H](NS(=O)(=O)NC2CCCCC2)C(c2ccccc2)c2ccccc2)cc1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL1159685
Phase Preclinical
Structure Type MOL
InChI Key IZMBGQNSYLZRGQ-GEEUVROYSA-N
Parent Compound CHEMBL1199308
Active Moiety CHEMBL1199308
1
Targets
2
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

630.8
MW (Da)
3.54
ALogP
5
HBA
5
HBD
157.5
PSA (Ų)
0.15
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H43F3N6O6S
MW 744.84
Aromatic Rings 3
Heavy Atoms 45
NP-Likeness -0.69

Activity Summary

Ki 2 meas. best 9.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine protease 1
CHEMBL3769
Ki 9.6 9.6 0.2 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 475.57 nM Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine protease 1 Ki = 0.25 nM 9.6 Binding affinity against bovine trypsin 11909707

Literature References

PubMed DOI Target Context # Activities
11909707 10.1016/s0960-894x(02)00093-8 Prothrombin 1
11909707 10.1016/s0960-894x(02)00093-8 Serine protease 1 1
11909707 10.1016/s0960-894x(02)00093-8 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine