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Compound Detail

CHEMBL205904

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CSc1sc(C(=N)N)cc1S(=O)(=O)c1cc(Br)c2c(c1)ncn2Cc1cc(F)ccc1F

Basic Information

ChEMBL ID CHEMBL205904
Phase Preclinical
Structure Type MOL
InChI Key HEZXZGJJNMPIJM-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

557.5
MW (Da)
5.03
ALogP
7
HBA
2
HBD
101.8
PSA (Ų)
0.20
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H15BrF2N4O2S3
MW 557.47
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.68

Activity Summary

Ki 3 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Complement C1s subcomponent
CHEMBL3913
Ki 8.0 8.0 10.0 1
Trypsin
CHEMBL2095204
Ki 5.85 5.85 1400.0 1
Coagulation factor X
CHEMBL244
Ki 4.94 4.94 11400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Complement C1s subcomponent Ki = 10.0 nM 8.0 Inhibition of C1S 16460935
Trypsin Ki = 1400.0 nM 5.85 Inhibition of trypsin 16460935
Coagulation factor X Ki = 11400.0 nM 4.94 Inhibition of F10a 16460935

Literature References

PubMed DOI Target Context # Activities
16460935 10.1016/j.bmcl.2006.01.036 Complement C1s subcomponent 1
16460935 10.1016/j.bmcl.2006.01.036 Urokinase-type plasminogen activator 1
16460935 10.1016/j.bmcl.2006.01.036 Tissue-type plasminogen activator 1
16460935 10.1016/j.bmcl.2006.01.036 Coagulation factor X 1
16460935 10.1016/j.bmcl.2006.01.036 Prothrombin 1
16460935 10.1016/j.bmcl.2006.01.036 Plasminogen 1
16460935 10.1016/j.bmcl.2006.01.036 Trypsin 1

Data from ChEMBL 36 via Core Engine