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Compound Detail

CHEMBL1159689

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N=C(N)c1ccc(CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Nc2ccccc2)C(c2ccccc2)c2ccccc2)cc1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL1159689
Phase Preclinical
Structure Type MOL
InChI Key BEDRUHFCUYFKFI-GEEUVROYSA-N
Parent Compound CHEMBL1200082
Active Moiety CHEMBL1200082
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

545.7
MW (Da)
4.89
ALogP
4
HBA
4
HBD
111.3
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 C36H36F3N5O4
MW 659.71
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -0.60

Activity Summary

Ki 2 meas. best 10.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 10.35 10.35 0.0 1
Serine protease 1
CHEMBL3769
Ki 8.82 8.82 1.5 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 53000.0 ng.hr.mL-1 Rattus norvegicus
Cmax 549.76 nM Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 0.045 nM 10.35 Binding affinity against human thrombin 11909707
Serine protease 1 Ki = 1.5 nM 8.82 Binding affinity against bovine trypsin 11909707

Literature References

PubMed DOI Target Context # Activities
11909707 10.1016/s0960-894x(02)00093-8 Rattus norvegicus 2
11909707 10.1016/s0960-894x(02)00093-8 Prothrombin 1
11909707 10.1016/s0960-894x(02)00093-8 Serine protease 1 1

Data from ChEMBL 36 via Core Engine