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Compound Detail

CHEMBL346857

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N=C(N)c1cccc(-n2nc(C(F)(F)F)cc2C(=O)Nc2ncc(-c3ccccc3S(N)(=O)=O)cn2)c1

Basic Information

ChEMBL ID CHEMBL346857
Phase Preclinical
Structure Type MOL
InChI Key CMCYVWKFRRVLKG-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

530.5
MW (Da)
2.53
ALogP
8
HBA
4
HBD
182.7
PSA (Ų)
0.22
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H17F3N8O3S
MW 530.49
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -1.60

Activity Summary

Ki 3 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypsin
CHEMBL2095204
Ki 7.7 7.7 20.0 1
Prothrombin
CHEMBL204
Ki 6.05 6.05 900.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 5.5 mL.min-1.kg-1 Canis lupus familiaris
T1/2 1.4 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypsin Ki = 20.0 nM 7.7 In vitro activity against human trypsin. 11170646
Prothrombin Ki = 900.0 nM 6.05 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 Homo sapiens 1

Data from ChEMBL 36 via Core Engine