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Compound Detail

CHEMBL440733

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Cc1cc(C(=O)Nc2ccc(-c3ccccc3S(C)(=O)=O)cc2)n(-c2cccc(C(=N)N)c2)n1

Basic Information

ChEMBL ID CHEMBL440733
Phase Preclinical
Structure Type MOL
InChI Key WQBWJCOPHBBJEE-UHFFFAOYSA-N
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

473.6
MW (Da)
3.79
ALogP
6
HBA
3
HBD
130.9
PSA (Ų)
0.29
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H23N5O3S
MW 473.56
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.70

Activity Summary

Ki 3 meas. best 7.89
IC50 1 meas.

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypsin
CHEMBL2095204
Ki 7.89 7.89 13.0 1
Prothrombin
CHEMBL204
Ki 6.75 6.75 180.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypsin Ki = 13.0 nM 7.89 In vitro activity against human trypsin. 11170646
Prothrombin Ki = 180.0 nM 6.75 In vitro activity against human thrombin. 11170646

Literature References

PubMed DOI Target Context # Activities
11170646 10.1021/jm000409z Coagulation factor X 1
11170646 10.1021/jm000409z Prothrombin 1
11170646 10.1021/jm000409z Trypsin 1
- 10.1039/C1MD00213A Coagulation factor X 1

Data from ChEMBL 36 via Core Engine