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Compound Detail

CHEMBL1200600

FLUOROMETHOLONE
💊 Approved Drug
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💊 Approved Drug
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ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL1200600
Name FLUOROMETHOLONE
Phase Approved
Structure Type MOL
InChI Key FAOZLTXFLGPHNG-KNAQIMQKSA-N
Therapeutic ✓ Yes

Known Names

Fluaton Fluor-op Fluorometholone Fluorometholone component of fml-s Fluorometolona Fml Fml forte Fml fte Fml-neo NSC-33001 Oxylone
5
Targets
11
Activities
3
Assay Types
0
PK Parameters
20
Publications
11
Known Names
6
Indications
1
Mechanisms

Molecular Properties

376.5
MW (Da)
2.92
ALogP
4
HBA
2
HBD
74.6
PSA (Ų)
0.74
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 1972
Availability Prescription
Chirality Single Enantiomer

Routes of Administration

Topical
USAN Stem -olone

Extended Properties

Molecular Formula C22H29FO4
MW 376.47
Aromatic Rings 0
Heavy Atoms 27
NP-Likeness 2.12

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Glucocorticoid receptor agonist AGONIST Glucocorticoid receptor ✓ ✓

Indications

Acne Vulgaris Eye Diseases Hemorrhoids Inflammation Dry Eye Syndromes Corneal Opacity

ATC Classification

C05AA06
fluorometholone
Level 1: CARDIOVASCULAR SYSTEM
Level 2: VASOPROTECTIVES
D07AB06
fluorometholone
Level 1: DERMATOLOGICALS
Level 2: CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
D07XB04
fluorometholone
Level 1: DERMATOLOGICALS
Level 2: CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
D10AA01
fluorometholone
Level 1: DERMATOLOGICALS
Level 2: ANTI-ACNE PREPARATIONS
S01BA07
fluorometholone
Level 1: SENSORY ORGANS
Level 2: OPHTHALMOLOGICALS
S01CB05
fluorometholone
Level 1: SENSORY ORGANS
Level 2: OPHTHALMOLOGICALS

Activity Summary

EC50 4 meas. best 6.4
IC50 4 meas. best 8.46
Ki 3 meas. best 8.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glucocorticoid receptor
CHEMBL2034
 Ki 8.8 8.8 1.6 1
Glucocorticoid receptor
CHEMBL2034
 IC50 8.46 8.46 3.5 1
Progesterone receptor
CHEMBL1909044
 Ki 6.97 6.97 106.0 1
Nuclear receptor subfamily 1 group I member 2
CHEMBL2146315
 EC50 6.4 6.4 400.0 1
Progesterone receptor
CHEMBL1909044
 IC50 6.09 6.09 815.0 1
Androgen receptor
CHEMBL3072
 Ki 6.07 6.07 857.0 1
Androgen receptor
CHEMBL3072
 IC50 5.89 5.89 1285.0 1
Nuclear receptor subfamily 1 group I member 2
CHEMBL3401
 EC50 5.89 5.43 1300.0 3

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Glucocorticoid receptor Ki = 1.578 nM 8.8 DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) -
Glucocorticoid receptor IC50 = 3.471 nM 8.46 DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) -
Progesterone receptor Ki = 106.0 nM 6.97 DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) -
Nuclear receptor subfamily 1 group I member 2 EC50 = 400.0 nM 6.4 Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase ... 20966043
Progesterone receptor IC50 = 815.0 nM 6.09 DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) -
Androgen receptor Ki = 857.0 nM 6.07 DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Miboler... -
Nuclear receptor subfamily 1 group I member 2 EC50 = 1300.0 nM 5.89 Competitive binding affinity to human PXR LBD (111 to 434) by TR-FRET assay 20966043
Androgen receptor IC50 = 1285.0 nM 5.89 DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Miboler... -
Nuclear receptor subfamily 1 group I member 2 EC50 = 3200.0 nM 5.5 Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induc... 20966043
Nuclear receptor subfamily 1 group I member 2 EC50 = 12600.0 nM 4.9 Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by l... 20966043

Literature References

PubMed DOI Target Context # Activities
22194678 10.1371/journal.pcbi.1002310 Hepatotoxicity 14
20966043 10.1124/dmd.110.035105 Nuclear receptor subfamily 1 group I member 2 8
37468498 10.1038/s41467-023-40064-9 Alpha-1A adrenergic receptor 3
37468498 10.1038/s41467-023-40064-9 Cannabinoid receptor 1 3
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
37468498 10.1038/s41467-023-40064-9 Gamma-aminobutyric acid receptor subunit alpha-1 2
37468498 10.1038/s41467-023-40064-9 Muscarinic acetylcholine receptor M2 2
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 2B 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
37468498 10.1038/s41467-023-40064-9 Alpha-2A adrenergic receptor 2
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 2A 2
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 1
37468498 10.1038/s41467-023-40064-9 Voltage-gated inwardly rectifying potassium channel KCNH2 1
37468498 10.1038/s41467-023-40064-9 Voltage-dependent L-type calcium channel subunit alpha-1C 1
37468498 10.1038/s41467-023-40064-9 Glutamate receptor ionotropic, NMDA 1 1
22961681 10.1124/dmd.112.047068 Bile salt export pump 1
37468498 10.1038/s41467-023-40064-9 Sodium-dependent dopamine transporter 1
- 10.6019/CHEMBL3301361 No relevant target 1
38318365 10.1016/j.isci.2024.108907 Deoxynucleoside triphosphate triphosphohydrolase SAMHD1 1

Data from ChEMBL 36 via Core Engine