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Compound Detail

CHEMBL93854

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COc1ccc2ccc(S(=O)(=O)N[C@H]3CCN(Cc4cc(C(=N)N)ccc4O)C3=O)cc2c1

Basic Information

ChEMBL ID CHEMBL93854
Phase Preclinical
Structure Type MOL
InChI Key WYPLWOJSDQFHPG-FQEVSTJZSA-N
7
Targets
9
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

468.5
MW (Da)
1.92
ALogP
6
HBA
4
HBD
145.8
PSA (Ų)
0.31
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H24N4O5S
MW 468.54
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.69

Activity Summary

Ki 9 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 8.52 8.52 3.0 2
Prothrombin
CHEMBL204
Ki 6.69 6.69 206.0 2
Serine protease 1
CHEMBL209
Ki 6.52 6.52 305.0 1
Trypsin II
CHEMBL4472
Ki 6.52 6.52 305.0 1
Tissue-type plasminogen activator
CHEMBL1873
Ki 5.97 5.97 1070.0 1
Vitamin K-dependent protein C
CHEMBL4444
Ki 5.71 5.71 1970.0 1
Plasminogen
CHEMBL1801
Ki 5.63 5.63 2350.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10479289 10.1021/jm990041+ Coagulation factor X 6
10509929 10.1016/s0960-894x(99)00466-7 Coagulation factor X 1
10509929 10.1016/s0960-894x(99)00466-7 Prothrombin 1
10509929 10.1016/s0960-894x(99)00466-7 Serine protease 1 1
10509929 10.1016/s0960-894x(99)00466-7 Vitamin K-dependent protein C 1
10509929 10.1016/s0960-894x(99)00466-7 Plasminogen 1
10509929 10.1016/s0960-894x(99)00466-7 Tissue-type plasminogen activator 1
10479289 10.1021/jm990041+ Prothrombin 1
10479289 10.1021/jm990041+ Trypsin II 1
10479289 10.1021/jm990041+ No relevant target 1
10479289 10.1021/jm990041+ Tissue factor 1

Data from ChEMBL 36 via Core Engine