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Compound Detail

CHEMBL4095408

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Cc1cccc(N(CCC(=O)O)C(=O)c2ccc3c(c2)nc(CNc2ccc(C(=N)N)cc2F)n3C)c1C

Basic Information

ChEMBL ID CHEMBL4095408
Phase Preclinical
Structure Type MOL
InChI Key GJBKRIOYAQUYEB-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

516.6
MW (Da)
4.35
ALogP
6
HBA
4
HBD
137.3
PSA (Ų)
0.19
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H29FN6O3
MW 516.58
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.72

Activity Summary

IC50 1 meas. best 8.81

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
IC50 8.81 8.81 1.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin IC50 = 1.54 nM 8.81 Inhibition of human thrombin preincubated for 10 mins followed by Ac-FVR-AMC sub... 27951488

Literature References

PubMed DOI Target Context # Activities
27951488 10.1016/j.ejmech.2016.12.015 Prothrombin 2
27951488 10.1016/j.ejmech.2016.12.015 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine