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Compound Detail

CHEMBL154322

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Cc1cc(C(=O)Nc2ccc(-c3ccccc3S(N)(=O)=O)cn2)n(-c2cccc(C(=N)N)c2)n1

Basic Information

ChEMBL ID CHEMBL154322
Phase Preclinical
Structure Type MOL
InChI Key DXVUPJDYIURFMP-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
3
PK Parameters
6
Publications
0
Known Names

Molecular Properties

475.5
MW (Da)
2.43
ALogP
7
HBA
4
HBD
169.8
PSA (Ų)
0.25
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 C23H21N7O3S
MW 475.53
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.80

Activity Summary

Ki 3 meas. best 7.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypsin
CHEMBL2095204
Ki 7.23 7.23 59.0 1
Prothrombin
CHEMBL204
Ki 5.85 5.85 1400.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 12.67 mL.min-1.kg-1 Canis lupus familiaris
F 1.0 % Canis lupus familiaris
T1/2 0.31 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypsin Ki = 59.0 nM 7.23 In vitro activity against human trypsin. 11170646
Prothrombin Ki = 1400.0 nM 5.85 In vitro activity against human thrombin. 11170646

Literature References

PubMed DOI Target Context # Activities
11170646 10.1021/jm000409z Canis familiaris 3
11170646 10.1021/jm000409z Coagulation factor X 1
11170646 10.1021/jm000409z Prothrombin 1
11170646 10.1021/jm000409z Trypsin 1
11170646 10.1021/jm000409z ADMET 1
11170646 10.1021/jm000409z Oryctolagus cuniculus 1

Data from ChEMBL 36 via Core Engine