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Compound Detail

CHEMBL327601

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CC(C)(C)OC(=O)N[C@@H](C(=O)N1CCC[C@H]1C(=O)NCC#Cc1c[nH]cn1)C(c1ccccc1)c1ccccc1

Basic Information

ChEMBL ID CHEMBL327601
Phase Preclinical
Structure Type MOL
InChI Key NGYNURMBAPAHLC-AHKZPQOWSA-N
2
Targets
2
Activities
1
Assay Types
3
PK Parameters
4
Publications
0
Known Names

Molecular Properties

541.6
MW (Da)
3.59
ALogP
5
HBA
3
HBD
116.4
PSA (Ų)
0.40
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H35N5O4
MW 541.65
Aromatic Rings 3
Heavy Atoms 40
NP-Likeness -0.63

Activity Summary

Ki 2 meas. best 7.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 7.62 7.62 24.0 1
Serine protease 1
CHEMBL3769
Ki 7.3 7.3 50.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 15707.85 ng.hr.mL-1 Rattus norvegicus
Cmax 14600.0 nM Rattus norvegicus
Tmax 1.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 24.0 nM 7.62 In vitro inhibition of human thrombin. 11133089
Serine protease 1 Ki = 50.0 nM 7.3 Inhibitory activity against Bovine Trypsin 11133089

Literature References

PubMed DOI Target Context # Activities
11133089 10.1016/s0960-894x(00)00579-5 Rattus norvegicus 3
11133089 10.1016/s0960-894x(00)00579-5 Prothrombin 1
11133089 10.1016/s0960-894x(00)00579-5 Serine protease 1 1
11133089 10.1016/s0960-894x(00)00579-5 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine