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Compound Detail

CHEMBL143421

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Cc1nc(N)ccc1CNC(=O)Cn1c(C)cnc(NCCc2ccncc2)c1=O

Basic Information

ChEMBL ID CHEMBL143421
Phase Preclinical
Structure Type MOL
InChI Key AEEBLJJSCIGASF-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

407.5
MW (Da)
1.20
ALogP
8
HBA
3
HBD
127.8
PSA (Ų)
0.51
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H25N7O2
MW 407.48
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.33

Activity Summary

Ki 2 meas. best 8.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 8.8 8.8 1.6 1
Serine protease 1
CHEMBL209
Ki 5.34 5.34 4600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 1.6 nM 8.8 Inhibitory constant against thrombin (IIa) 12570369
Serine protease 1 Ki = 4600.0 nM 5.34 Inhibitory constant against human trypsin 12570369

Literature References

PubMed DOI Target Context # Activities
12570369 10.1021/jm020311f Prothrombin 1
12570369 10.1021/jm020311f Serine protease 1 1
12570369 10.1021/jm020311f NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine