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Compound Detail

CHEMBL523854

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CCNC(=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(F)c2)cn1

Basic Information

ChEMBL ID CHEMBL523854
Phase Preclinical
Structure Type MOL
InChI Key IQTIQAPIFLPGHQ-QHNZEKIYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

491.6
MW (Da)
5.20
ALogP
4
HBA
2
HBD
80.3
PSA (Ų)
0.56
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H34FN3O3
MW 491.61
Aromatic Rings 2
Heavy Atoms 36
NP-Likeness -0.27

Activity Summary

Ki 1 meas. best 8.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proteinase-activated receptor 1
CHEMBL3974
Ki 8.32 8.32 4.8 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Proteinase-activated receptor 1 Ki = 4.8 nM 8.32 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