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Compound Detail

CHEMBL345990

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COC(=O)C1C/C(=C\c2ccc(C(=N)N)cc2)C(=O)/C(=C/c2ccc(C(=N)N)cc2)C1

Basic Information

ChEMBL ID CHEMBL345990
Phase Preclinical
Structure Type MOL
InChI Key DFAIXITYTZBSLF-XOBNHNQQSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

416.5
MW (Da)
2.87
ALogP
5
HBA
4
HBD
143.1
PSA (Ų)
0.26
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H24N4O3
MW 416.48
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness 0.03

Activity Summary

Ki 2 meas. best 7.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine protease 1
CHEMBL3769
Ki 7.14 7.14 72.0 1
Prothrombin
CHEMBL204
Ki 5.36 5.36 4400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine protease 1 Ki = 72.0 nM 7.14 In vitro inhibition of bovine trypsin(Trp). 10639283
Prothrombin Ki = 4400.0 nM 5.36 In vitro inhibition of human thrombin(FIIa). 10639283

Literature References

PubMed DOI Target Context # Activities
10639283 10.1021/jm990456v Coagulation factor X 1
10639283 10.1021/jm990456v Prothrombin 1
10639283 10.1021/jm990456v Serine protease 1 1

Data from ChEMBL 36 via Core Engine