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Compound Detail

CHEMBL137945

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NCCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CC1CCCCC1)NCC(=O)O)C(=O)c1nccs1

Basic Information

ChEMBL ID CHEMBL137945
Phase Preclinical
Structure Type BOTH
InChI Key GBGSLJOXHGXFTF-ZCNNSNEGSA-N
1
Targets
2
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

521.7
MW (Da)
1.94
ALogP
8
HBA
4
HBD
154.7
PSA (Ų)
0.21
QED
1
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H39N5O5S
MW 521.68
Aromatic Rings 1
Heavy Atoms 36
NP-Likeness -0.22

Activity Summary

Ki 2 meas. best 8.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 8.59 8.59 2.6 2

Pharmacokinetic Data

Parameter Value Units Species
F 11.0 % Eutheria
T1/2 0.3833 hr -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 2.6 nM 8.59 Inhibitory activity against thrombin. 12238922
Prothrombin Ki = 2.6 nM 8.59 Inhibition of human alpha-thrombin 18053726

Literature References

PubMed DOI Target Context # Activities
12238922 10.1021/jm011110z Prothrombin 2
12238922 10.1021/jm011110z ADMET 2
18053726 10.1016/j.bmc.2007.11.015 Prothrombin 1

Data from ChEMBL 36 via Core Engine