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Compound Detail

CHEMBL370579

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CC1CCCN(c2c(C#N)c(C(F)F)nn2-c2ccc(S(C)(=O)=O)cn2)C1

Basic Information

ChEMBL ID CHEMBL370579
Phase Preclinical
Structure Type MOL
InChI Key BGGLZGWRRYHVLQ-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
4
PK Parameters
6
Publications
0
Known Names

Molecular Properties

395.4
MW (Da)
2.72
ALogP
7
HBA
0
HBD
91.9
PSA (Ų)
0.79
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 C17H19F2N5O2S
MW 395.44
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -1.98

Activity Summary

IC50 4 meas. best 7.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclooxygenase-2
CHEMBL4033
IC50 7.52 7.52 30.0 1
Unchecked
CHEMBL612545
IC50 7.52 6.52 30.0 2
Prostaglandin G/H synthase 1
CHEMBL4133
IC50 5.7 5.7 2000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 450000000000.0 ng.hr.mL-1 Canis lupus familiaris
Cmax 381.85 nM Canis lupus familiaris
T1/2 4.6 hr Canis lupus familiaris
Tmax 0.5 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16275075 10.1016/j.bmcl.2005.10.006 Canis familiaris 4
17126015 10.1016/j.bmcl.2006.11.026 Unchecked 4
16275075 10.1016/j.bmcl.2005.10.006 Prostaglandin G/H synthase 1 1
16275075 10.1016/j.bmcl.2005.10.006 Cyclooxygenase-2 1
16275075 10.1016/j.bmcl.2005.10.006 Unchecked 1
17126015 10.1016/j.bmcl.2006.11.026 No relevant target 1

Data from ChEMBL 36 via Core Engine