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Compound Detail

CHEMBL460583

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CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(N)=O)c2)cn1

Basic Information

ChEMBL ID CHEMBL460583
Phase Preclinical
Structure Type MOL
InChI Key UTNWIKJEISYSBD-GCYZNPIISA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

517.6
MW (Da)
4.59
ALogP
6
HBA
2
HBD
120.6
PSA (Ų)
0.54
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H35N3O5
MW 517.63
Aromatic Rings 2
Heavy Atoms 38
NP-Likeness -0.01

Activity Summary

Ki 1 meas. best 6.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proteinase-activated receptor 1
CHEMBL3974
Ki 6.43 6.43 367.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Proteinase-activated receptor 1 Ki = 367.0 nM 6.43 Displacement of [3H]haTRAP from PAR1 in human platelets 18447380

Literature References

PubMed DOI Target Context # Activities
18447380 10.1021/jm800180e Proteinase-activated receptor 1 1

Data from ChEMBL 36 via Core Engine