niflumic acid 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
anti-inflammatory, anilinonicotinic acid derivatives 1925 4394-00-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • niflumic acid
  • niflamol
  • nifluminic acid
An analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis.
  • Molecular weight: 282.22
  • Formula: C13H9F3N2O2
  • CLOGP: 4.77
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 2
  • TPSA: 62.22
  • ALOGS: -3.50
  • ROTB: 4

Drug dosage:

DoseUnitRoute
0.75 g O

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.183 Moderate 0.74
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.816 Moderate 0.74
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 86.099 10^-6 cm/s Moderate 0.74
dh-clint Dog hepatocyte intrinsic clearance 6.887 uL/min/10^6 cells Moderate 0.74
dppb Dog plasma protein binding (% unbound) 0.720 % Moderate 0.74
fcs-ppb Fetal calf serum protein binding (% unbound) 1.080 % Moderate 0.74
herg hERG pIC50 4.365 pIC50 Moderate 0.74
hh-clint Human hepatocyte intrinsic clearance 11.776 uL/min/10^6 cells Moderate 0.74
hlm-clint Human liver microsomal intrinsic clearance 4.989 uL/min/mg protein Moderate 0.74
hppb Human plasma protein binding (% unbound) 0.440 % Moderate 0.74
kinase-safety-class ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,IKBKB,MAPK7,PDK1,PDK2,PDK4,PIK3CB,PRKDC,STK33,TEK 22
kinase-selectivity-class ACVR2B,AXL,BRAF,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,GRK2,MAPK7,SIK2,STK33,TTK 13
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 5.333 Moderate 0.74
mh-clint Mouse hepatocyte intrinsic clearance 21.878 Moderate 0.74
mppb Mouse plasma protein binding (% unbound) 1.960 Moderate 0.74
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 1.387 Moderate 0.74
pfas-class PFAS structural alert (1 = True, 0 = False) 1
pppb Pig plasma protein binding (% unbound) 1.160 % Moderate 0.74
rh-clint Rat hepatocyte intrinsic clearance 19.320 uL/min/10^6 cells Moderate 0.74
rh-fuinc Rat hepatocyte fraction unbound in incubation 51.730 % Moderate 0.74
rppb Rat plasma protein binding (% unbound) 0.520 % Moderate 0.74
solubility-dd Solubility at pH 7.4 in DMSO 918.333 uM Moderate 0.74

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Aspirin-exacerbated respiratory disease 71.27 62.35 9 136 939 110588215

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC M01AX02 MUSCULO-SKELETAL SYSTEM
ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS
ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS, NON-STEROIDS
Other antiinflammatory and antirheumatic agents, non-steroids
ATC M02AA17 MUSCULO-SKELETAL SYSTEM
TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN
TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN
Antiinflammatory preparations, non-steroids for topical use
MeSH PA D000700 Analgesics
MeSH PA D000893 Anti-Inflammatory Agents
MeSH PA D000894 Anti-Inflammatory Agents, Non-Steroidal
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D016861 Cyclooxygenase Inhibitors
MeSH PA D018501 Antirheumatic Agents
MeSH PA D018689 Sensory System Agents
MeSH PA D018712 Analgesics, Non-Narcotic

Related Drugs by ATC class:

M01AX Other antiinflammatory and antirheumatic agents, non-steroids 13 drugs
azapropazonebenzydaminechondroitin sulfatediacereinfeprazoneglucosaminemorniflumatenabumetonenimesulideorgoteinoxaceprolproquazone show all 13 →
M02AA Antiinflammatory preparations, non-steroids for topical use 28 drugs
aceclofenacbendazacbenzydaminebufexamacclofezonedexketoprofendiclofenacesflurbiprofenetofenamatefelbinacfentiazacfeprazone show all 28 →

Drug Use | Suggest Off label Use Form| |View source of the data|

None




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 1.74 acidic
pKa2 5.54 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Prostaglandin G/H synthase 2 Enzyme IC50 6.04 DRUG MATRIX
Prostaglandin G/H synthase 1 Enzyme IC50 5.97 DRUG MATRIX
Dihydroorotate dehydrogenase (quinone), mitochondrial Enzyme IC50 4.77 CHEMBL
Transthyretin Secreted Kd 6.59 CHEMBL
Chloride channel protein ClC-Ka Ion channel ACTIVATOR EC50 5 IUPHAR
Potassium channel subfamily T member 2 Ion channel ACTIVATOR EC50 8.68 IUPHAR
G-protein coupled receptor 35 GPCR Ki 5.44 CHEMBL
Chloride channel protein ClC-Kb Ion channel ACTIVATOR EC50 5 IUPHAR
Transcriptional enhancer factor TEF-3 Transcription factor Kd 4.55 CHEMBL
Transcription factor SOX-18 Transcription factor IC50 4.30 CHEMBL

External reference:

IDSource
N0000167326 NUI
D08275 KEGG_DRUG
C0028067 UMLSCUI
CHEBI:34888 CHEBI
NFL PDB_CHEM_ID
CHEMBL63323 ChEMBL_ID
DB04552 DRUGBANK_ID
D009544 MESH_DESCRIPTOR_UI
4488 PUBCHEM_CID
2439 IUPHAR_LIGAND_ID
2194 INN_ID
4U5MP5IUD8 UNII
7418 RXNORM
005830 NDDF
494421000221106 SNOMEDCT_US
4U5MP5IUD8 INXIGHT DRUGS

Pharmaceutical products:

None