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Compound Detail

CHEMBL745

PRIMARY ALCOHOL METABOLITE OF CELECOXIB
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NS(=O)(=O)c1ccc(-n2nc(C(F)(F)F)cc2-c2ccc(CO)cc2)cc1

Basic Information

ChEMBL ID CHEMBL745
Name PRIMARY ALCOHOL METABOLITE OF CELECOXIB
Phase Preclinical
Structure Type MOL
InChI Key ICRSYPPLGADZKA-UHFFFAOYSA-N
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

397.4
MW (Da)
2.70
ALogP
5
HBA
2
HBD
98.2
PSA (Ų)
0.71
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 C17H14F3N3O3S
MW 397.38
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.21

Activity Summary

IC50 5 meas. best 5.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prostaglandin G/H synthase 2
CHEMBL4102
IC50 5.43 5.43 3700.0 1
Prostaglandin G/H synthase 1
CHEMBL2949
IC50 5.15 5.15 7100.0 1
Prostaglandin G/H synthase 2
CHEMBL230
IC50 4.03 4.03 93300.0 2
Prostaglandin G/H synthase 2
CHEMBL4321
IC50 4.03 4.03 93325.4 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12383007 10.1021/jm020089e Prostaglandin G/H synthase 1 2
12383007 10.1021/jm020089e Prostaglandin G/H synthase 2 2
11412976 10.1016/s0960-894x(00)00522-9 Prostaglandin G/H synthase 1 1
11412976 10.1016/s0960-894x(00)00522-9 Prostaglandin G/H synthase 2 1
11814774 10.1016/s0960-894x(01)00825-3 Prostaglandin G/H synthase 2 1
9135032 10.1021/jm960803q Prostaglandin G/H synthase 1 1
9135032 10.1021/jm960803q Prostaglandin G/H synthase 2 1
12383007 10.1021/jm020089e Unchecked 1
18930406 10.1016/j.bmc.2008.10.001 Prostaglandin G/H synthase 1 1
18930406 10.1016/j.bmc.2008.10.001 Prostaglandin G/H synthase 2 1
18930406 10.1016/j.bmc.2008.10.001 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine