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Compound Detail

CHEMBL190083

TARENFLURBIL
🧪 Phase III
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🧪 Phase III
C[C@@H](C(=O)O)c1ccc(-c2ccccc2)c(F)c1
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL190083
Name TARENFLURBIL
Phase Phase III
Structure Type MOL
InChI Key SYTBZMRGLBWNTM-SNVBAGLBSA-N

Known Names

E-7869 Flurbiprofen, (r)- MPC-7869 R-flurbiprofen Tarenflurbil Tarenflurbilo
4
Targets
12
Activities
2
Assay Types
1
PK Parameters
20
Publications
6
Known Names
3
Indications
1
Mechanisms

Molecular Properties

244.3
MW (Da)
3.68
ALogP
1
HBA
1
HBD
37.3
PSA (Ų)
0.89
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer
USAN Year 2005

Extended Properties

Molecular Formula C15H13FO2
MW 244.26
Aromatic Rings 2
Heavy Atoms 18
NP-Likeness -0.43

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Gamma-secretase modulator MODULATOR Gamma-secretase ✓ ✓

Indications

Alzheimer Disease Dementia Prostatic Neoplasms, Castration-Resistant

Activity Summary

IC50 10 meas. best 5.89
EC50 2 meas.

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prostaglandin G/H synthase 2
CHEMBL4321
 IC50 5.89 5.89 1300.0 1
Prostaglandin G/H synthase 1
CHEMBL221
 IC50 4.36 4.36 44000.0 1
Prostaglandin G/H synthase 1
CHEMBL4042
 IC50 4.36 4.36 44000.0 1
Gamma-secretase
CHEMBL2094135
 IC50 4.0 4.0 100000.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 92.0 % Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prostaglandin G/H synthase 2 IC50 = 1300.0 nM 5.89 Inhibition of COX2-mediated 2-arachidonoylglycerol oxygenation in LPS/IFN-gamma-... 22984634
Prostaglandin G/H synthase 1 IC50 = 44000.0 nM 4.36 Concentration required to inhibit cyclooxygenase-1 in rat blood 16134939
Prostaglandin G/H synthase 1 IC50 = 44000.0 nM 4.36 Inhibition of COX1 in human whole blood 16455248
Gamma-secretase IC50 = 100000.0 nM 4.0 Modulation of gamma secretase (unknown origin) assessed as reduction in amyloid ... 27045975

Literature References

PubMed DOI Target Context # Activities
16455248 10.1016/j.bmcl.2006.01.033 Mus musculus 3
22984634 10.1021/ml3001616 Prostaglandin G/H synthase 2 2
22984634 10.1021/ml3001616 Plasma 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
- 10.6019/CHEMBL4651402 SARS-CoV-2 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
19694467 10.1021/jm900188z Unchecked 1
21141968 10.1021/jm101168r Brain 1
24900267 10.1021/ml200175q Unchecked 1
22061640 10.1016/j.bmcl.2011.10.047 Unchecked 1
20503989 10.1021/jm1003073 Unchecked 1
20503989 10.1021/jm1003073 Prostaglandin G/H synthase 1 1
20503989 10.1021/jm1003073 Prostaglandin G/H synthase 2 1
15974585 10.1021/jm049082i Interleukin-8 receptors, CXCR1/CXCR2 1
16455248 10.1016/j.bmcl.2006.01.033 Prostaglandin G/H synthase 1 1
16455248 10.1016/j.bmcl.2006.01.033 Unchecked 1
16455248 10.1016/j.bmcl.2006.01.033 Gamma-secretase 1
16134939 10.1021/jm0502541 Prostaglandin G/H synthase 2 1
16134939 10.1021/jm0502541 Prostaglandin G/H synthase 1 1
16134939 10.1021/jm0502541 Amyloid-beta precursor protein 1

Data from ChEMBL 36 via Core Engine