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Compound Detail

CHEMBL443302

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COc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(C)(=O)=O)cn2)cc1Cl

Basic Information

ChEMBL ID CHEMBL443302
Phase Preclinical
Structure Type MOL
InChI Key NZWVOYGBWIEMSS-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
4
Publications
0
Known Names

Molecular Properties

431.8
MW (Da)
4.02
ALogP
6
HBA
0
HBD
74.1
PSA (Ų)
0.62
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H13ClF3N3O3S
MW 431.82
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.81

Activity Summary

IC50 1 meas. best 6.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclooxygenase-2
CHEMBL4033
IC50 6.52 6.52 300.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 115.0 ng.hr.mL-1 Canis lupus familiaris
Cmax 97.26 nM Canis lupus familiaris
T1/2 2.6 hr Canis lupus familiaris
Tmax 0.8 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclooxygenase-2 IC50 = 300.0 nM 6.52 In vitro inhibitory activity against canine prostaglandin G/H synthase 2. 14684306

Literature References

PubMed DOI Target Context # Activities
14684306 10.1016/j.bmcl.2003.10.004 Canis familiaris 5
14684306 10.1016/j.bmcl.2003.10.004 Prostaglandin G/H synthase 1 1
14684306 10.1016/j.bmcl.2003.10.004 Cyclooxygenase-2 1
14684306 10.1016/j.bmcl.2003.10.004 Unchecked 1

Data from ChEMBL 36 via Core Engine