All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

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

Stem definition	Drug id	CAS RN
antipsychotics, haloperidol derivatives	407	10457-90-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: bromperidol hydrochloride bromperidol HCl tesoprel bromperidol azurene bromoperidol impromen	bromine-substituted for chlorine in haloperidol; RN given refers to unlabeled parent cpd; structure Molecular weight: 420.32 Formula: C21H23BrFNO2 CLOGP: 4 LIPINSKI: 0 HAC: 3 HDO: 1 TPSA: 40.54 ALOGS: -4.76 ROTB: 6

Drug dosage:

Dose	Unit	Route
10	mg	O
10	mg	P
3.30	mg	P

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.09 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.98 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	50 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
azlogd74	LogD at pH 7.4	3.034		High	0.83
caco2-efflux	Caco-2 efflux ratio (BA/AB)	0.698		High	0.83
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	29.444	10^-6 cm/s	High	0.83
dh-clint	Dog hepatocyte intrinsic clearance	15.959	uL/min/10^6 cells	High	0.83
dppb	Dog plasma protein binding (% unbound)	11.650	%	High	0.83
fcs-ppb	Fetal calf serum protein binding (% unbound)	34.160	%	High	0.83
herg	hERG pIC50	6.782	pIC50	High	0.83
hh-clint	Human hepatocyte intrinsic clearance	2.360	uL/min/10^6 cells	High	0.83
hlm-clint	Human liver microsomal intrinsic clearance	14.421	uL/min/mg protein	High	0.83
hppb	Human plasma protein binding (% unbound)	11.230	%	High	0.83
kinase-safety-class	ACVR2A,ACVR2B,AKT1,AKT2,AKT3,ALK,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK1,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK	52
kinase-selectivity-class	AKT2,AKT3,AXL,EIF2AK3,GRK2,PDK4,PRKCD,SIK2	8
mdck-mdr1-bcrp-efflux	MDCK-MDR1-BCRP efflux ratio	0.389		High	0.83
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	0.598		High	0.83
mh-clint	Mouse hepatocyte intrinsic clearance	23.442		High	0.83
mppb	Mouse plasma protein binding (% unbound)	12.250		High	0.83
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	1.820		High	0.83
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
pld-class	Phospholipidosis risk class (1 = positive, 0 = negative)	1		High	0.83
rat-kpuu-brain	Rat brain Kpuu	0.068	%	High	0.83
pppb	Pig plasma protein binding (% unbound)	23.440	%	High	0.83
rh-clint	Rat hepatocyte intrinsic clearance	53.456	uL/min/10^6 cells	High	0.83
rh-fuinc	Rat hepatocyte fraction unbound in incubation	26.680	%	High	0.83
rppb	Rat plasma protein binding (% unbound)	9.960	%	High	0.83
solubility-dd	Solubility at pH 7.4 in DMSO	28.510	uM	High	0.83

Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1973	YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N05AD06	NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Butyrophenone derivatives
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D011619	Psychotropic Drugs
MeSH PA	D014149	Tranquilizing Agents
MeSH PA	D014150	Antipsychotic Agents
CHEBI has role	CHEBI:35469	antidepressant
CHEBI has role	CHEBI:35474	anxiolytic drug
CHEBI has role	CHEBI:35476	antipsychotic agent

Related Drugs by ATC class:

N05AD Butyrophenone derivatives 8 drugs

benperidoldroperidolhaloperidollumateperonemelperonemoperonepipamperonetrifluperidol

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 level	Dissociation constant	Type (acidic/basic)
pKa1	8.36	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	ANTAGONIST	Ki	8.43		WOMBAT-PK	KEGG DRUG
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		EC50	9.02		WOMBAT-PK
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	7.10		WOMBAT-PK
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	7.50		WOMBAT-PK
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN		Ki	6.16		WOMBAT-PK
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	5.12		PDSP
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN		Ki	5.75		PDSP
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN		Ki	5.15		PDSP
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN		Ki	5.77		PDSP
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN		Ki	5.32		PDSP
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	7		WOMBAT-PK
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN		Ki	7.80		WOMBAT-PK

External reference:

ID	Source
D01101	KEGG_DRUG
19777	RXNORM
C1369894	UMLSCUI
CHEBI:31305	CHEBI
CHEMBL28218	ChEMBL_ID
DB12401	DRUGBANK_ID
C006820	MESH_SUPPLEMENTAL_RECORD_UI
2448	PUBCHEM_CID
3737	INN_ID
LYH6F7I22E	UNII
725571009	SNOMEDCT_US
006754	NDDF
LYH6F7I22E	INXIGHT DRUGS

Pharmaceutical products:

None