OralParenteralDosed ingredientTherapeutic flag

Haloperidol

CAS 52-86-8

Haloperidol (CAS 52-86-8) is a Phase 4 pharmaceutical compound with 48 bioactivity targets and 2,675 adverse event associations.

SOURCE NLM DailyMed

Label records

SOURCE EMBL-EBI ChEMBL

Bioactivity

SOURCE DrugCentral / FAERS

Adverse signals

2,675

SOURCE IUPHAR / PharmGKB

PubMed IDs

SOURCE ChEMBL 36 B25820EEF0F0

Compound Identity

Matched identifiers and naming fields for the pharmaceutical compound record.

Primary Name

Haloperidol

CAS Number

52-86-8

UNII

J6292F8L3D

InChIKey

LNEPOXFFQSENCJ-UHFFFAOYSA-N

ChEMBL ID

CHEMBL54

Molecule Type

Small molecule

Source Match

EMBL-EBI ChEMBL (INCHIKEY)

Synonyms and normalized names

HALOPERIDOL DECANOATEhaloperidol lactateHaldol

black box warningdosed ingredientoralparenteraltherapeutic flag

SOURCE ChEMBL 36 B25820EEF0F0

Clinical Development Phase

Highest clinical development phase rendered from the matched compound identifier rows.

Phase 4 (Approved)

Approved or marketed human pharmaceutical use is represented in the source phase field.

ChEMBL CHEMBL54 | Small molecule

SOURCE ChEMBL 36 activities + assays 80 bioactivity rows

Bioactivity & Target Interactions

Target-level activity records with assay counts, activity type, and measured value where present.

Target	Activity	Value	Assays	Organism
-	Ki	404.21271789099524 nM	829	-
-	IC50	4078.638089803922 nM	247	-
-	AC50	16959.248639053254 nM	168	-
-	Potency	14189.426470588236 nM	66	-
-	GI50	34401.98072727273 nM	55	-
-	Kd	16681.804422222223 nM	9	-
-	EC50	10002.822857142857 nM	7	-
-	MIC	57300 nM	6	-
-	MIC	3.125 ug.mL-1	2	-
-	EC50	0.2 mg kg-1	1	-
-	EC50	0.88 umol/Kg	1	-
Calmodulin Cytosolic other	IC50	6.3	-	Homo sapiens
5-hydroxytryptamine receptor 5A GPCR	Ki	5.648	-	Homo sapiens
5-hydroxytryptamine receptor 1F GPCR	Ki	5.301	-	Homo sapiens
5-hydroxytryptamine receptor 1E GPCR	Ki	5.301	-	Homo sapiens
Beta-2 adrenergic receptor GPCR	Ki	5.301	-	Homo sapiens
Mu-type opioid receptor GPCR	Ki	6.003	-	Homo sapiens
D(1A) dopamine receptor GPCR	Ki	7.82	-	Homo sapiens
D(2) dopamine receptor GPCR	Ki	9.15	-	Homo sapiens
Alpha-2A adrenergic receptor GPCR	Ki	5.947	-	Homo sapiens
Sigma non-opioid intracellular receptor 1 Membrane receptor	EC50	8.92	-	Homo sapiens
Potassium voltage-gated channel subfamily H member 2 Ion channel	IC50	7.5	-	Homo sapiens
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase Enzyme	Ki	6.72	-	Homo sapiens
Multidrug resistance protein 1 Transporter	Ki	6.7	-	Homo sapiens
Sodium-dependent serotonin transporter Transporter	Ki	5.74	-	Homo sapiens
Sodium-dependent noradrenaline transporter Transporter	Ki	5.74	-	Homo sapiens
5-hydroxytryptamine receptor 1A GPCR	Ki	5.55	-	Homo sapiens
5-hydroxytryptamine receptor 2A GPCR	Ki	7	-	Homo sapiens
5-hydroxytryptamine receptor 2B GPCR	Ki	6.1	-	Homo sapiens
5-hydroxytryptamine receptor 2C GPCR	Ki	5.33	-	Homo sapiens
5-hydroxytryptamine receptor 6 GPCR	Ki	5.22	-	Homo sapiens
5-hydroxytryptamine receptor 7 GPCR	Ki	6.45	-	Homo sapiens
Alpha-1A adrenergic receptor GPCR	Ki	7.9	-	Homo sapiens
Alpha-2B adrenergic receptor GPCR	Ki	6.319	-	Homo sapiens
D(3) dopamine receptor GPCR	Ki	8.52	-	Homo sapiens
D(1B) dopamine receptor GPCR	Ki	7.52	-	Homo sapiens
Histamine H1 receptor GPCR	Ki	6.36	-	Homo sapiens
Histamine H2 receptor GPCR	Ki	5.999	-	Homo sapiens
Muscarinic acetylcholine receptor M1 GPCR	Ki	5.8	-	Homo sapiens
Muscarinic acetylcholine receptor M3 GPCR	Ki	5	-	Homo sapiens
Muscarinic acetylcholine receptor M5 GPCR	Ki	6.182	-	Homo sapiens
5-hydroxytryptamine receptor 1B GPCR	Ki	6.569	-	Homo sapiens
5-hydroxytryptamine receptor 1D GPCR	Ki	6.6	-	Homo sapiens
Alpha-2C adrenergic receptor GPCR	Ki	6.26	-	Homo sapiens
Alpha-1D adrenergic receptor GPCR	Ki	7.553	-	Homo sapiens
Alpha-1B adrenergic receptor GPCR	Ki	8.097	-	Homo sapiens
Potassium channel subfamily K member 2 Ion channel	IC50	5.26	-	Homo sapiens
Potassium voltage-gated channel subfamily H member 1 Ion channel	IC50	6.2	-	Homo sapiens
Alpha-1B adrenergic receptor GPCR	Ki	8.305	-	Rattus norvegicus
Membrane-associated progesterone receptor component 1 Membrane receptor	Ki	7.444	-	Rattus norvegicus

SOURCE DrugCentral 2023 / FAERS disproportionality 80 associations

Adverse Event Associations

DrugCentral / FAERS disproportionality signal rows matched to this compound.

Reaction PT	Drug AE	LLR	MedDRA
Neuroleptic malignant syndrome	1425	4095.68	10029282
Extrapyramidal disorder	1264	3616.483	10015832
Intentional self-injury	760	1522.98	10022524
Akathisia	560	1375.96	10001540
Dystonia	607	1347.992	10013983
Catatonia	358	937.235	10007776
Drug interaction	1680	930.408	10013710
Muscle rigidity	452	924.612	10028330
Agitation	800	841.141	10001497
Psychotic disorder	540	783.3	10061920
Parkinsonism	375	754.958	10034010
Sedation	569	738.531	10039897
Salivary hypersecretion	345	714.265	10039424
Delirium	655	689.458	10012218
Sopor	423	673.428	10058709
Electrocardiogram QT prolonged	658	656.819	10014387
Hyperprolactinaemia	228	615.854	10020737
Hallucination, auditory	355	612.717	10019070
Aggression	506	608.515	10001488
Tardive dyskinesia	299	606.19	10043118
Suicide attempt	613	587.261	10042464
Delusion	337	564.094	10012239
Arthralgia	93	496.722	10003239
Blood creatine phosphokinase increased	482	487.383	10005470
Somnolence	988	483.564	10041349
Intentional overdose	568	422.883	10022523
Pain	238	411.833	10033371
Schizophrenia	245	401.897	10039626
Fatigue	445	387.828	10016256
Weight increased	1038	381.21	10047899
Dyskinesia	362	370.388	10013916
Tachycardia	704	364.089	10043071
Rhabdomyolysis	505	363.604	10039020
Tremor	706	346.512	10044565
Restlessness	343	340.097	10038743
Psychomotor hyperactivity	224	327.084	10037211
Rash	210	322.578	10037844
Hypothermia	238	320.978	10021113
Headache	235	320.248	10019211
Joint swelling	25	320.147	10023232
Antipsychotic drug level below therapeutic	119	317.398	10060145
Coma	479	316.756	10010071
Toxicity to various agents	1107	307.316	10070863
Infusion related reaction	13	286.696	10051792
Rheumatoid arthritis	7	284.425	10039073
Torsade de pointes	205	281.537	10044066
Abnormal behaviour	282	269.177	10061422
Hypertonia	147	264.654	10020852
Overdose	647	258.448	10033295
Disinhibition	114	257.662	10013142

Association rows are source-linked signal records, not incidence rates or clinical causality claims.

SOURCE IUPHAR ligand-target interactions 19 interactions

IUPHAR Ligand-Target Data

Curated ligand-target interaction rows with action, affinity, and literature identifiers.

Target	Action	Affinity	PubMed
5-HT 2A receptor HTR2A	Antagonist	6.699999809265137 pKi	8935801\|9732398\|12629531\|15102927\|18308814
D 2 receptor DRD2	Antagonist	7.400000095367432 pKi	8301582\|7907989\|1354163\|7664822\|7862709
D 3 receptor DRD3	Antagonist	7.5 pKi	8301582\|1354163\|7862709\|18308814
D 4 receptor DRD4	Antagonist	8.699999809265137 pKi	8102973\|7862709\|18308814
5-HT 1A receptor HTR1A	Antagonist	5.7 pKi	9760039\|9067310\|8935801\|9732398
5-HT 1D receptor HTR1D	Antagonist	6.6 pKi	8935801
5-HT 2A receptor Htr2a	Antagonist	7.4 pKi	9655845
5-HT 2B receptor HTR2B	Antagonist	5.8 pKi	9459568
5-HT 7 receptor Htr7	Antagonist	6.3 pKi	8997630\|7908055\|8397408
5-HT 7 receptor HTR7	Antagonist	6.3 pKi	9298538
5-HT 7 receptor Htr7	Antagonist	6.3 pKi	8394987
D 1 receptor DRD1	Antagonist	7.599999904632568 pKi	1826762\|18308814
D 2 receptor Drd2	Antagonist	8.300000190734863 pKi	1975644
D 3 receptor Drd3	Antagonist	7.0 pKi	1975644
D 5 receptor DRD5	Antagonist	6.3 pKi	1826762
H 1 receptor HRH1	Antagonist	5.7 pKi	8935801\|12629531
K ir 3.2 Kcnj6	Antagonist	4.1 pEC50	10780978
K v 10.1 KCNH1	Channel blocker	6.2 pIC50	12522086
TAS2R10 TAS2R10	Agonist	-	20022913

SOURCE PharmGKB drug-gene phenotypes 60 phenotype rows

Pharmacogenomics

Drug-gene phenotype annotations and evidence levels from PharmGKB-mapped rows.

CYP2D6 (PA128) CYP2D6*1, CYP2D6*1xN

Evidence: -; PMID 22775532

CYP2D6 (PA128) CYP2D6*3, CYP2D6*4

Evidence: -; PMID 22775532

HTR2C (PA194) rs3813929

Evidence: -; PMID 21121776

HTR2C (PA194) rs3813929

Evidence: -; PMID 17702092

HTR2C (PA194) rs518147

Evidence: -; PMID 21121776

HTR2C (PA194) rs6318

Evidence: -; PMID 17702092

- rs7912580

Evidence: -; PMID 24751813

DTNBP1 (PA27512) rs909706

Evidence: -; PMID 19369910

CYP2D6 (PA128) CYP2D6*1, CYP2D6*10

Evidence: -; PMID 12919180

EIF2AK4 (PA134947616) rs2412459

Evidence: -; PMID 24751813

SLC6A5 (PA35911) rs2298826

Evidence: -; PMID 20859245

CYP2D6 (PA128) CYP2D6*1, CYP2D6*5

Evidence: -; PMID 9352580

ANKK1 (PA134872551) rs2587550

Evidence: -; PMID 22893251

CYP2D6 (PA128) CYP2D6*1, CYP2D6*10

Evidence: -; PMID 9352580

SLC6A4 (PA312) SLC6A4 HTTLPR long form (L allele), SLC6A4 HTTLPR short form (S allele)

Evidence: -; PMID 20031235

COMT (PA117) rs4680

Evidence: -; PMID 23963056

DRD2 (PA27478) rs1800497

Evidence: -; PMID 23963056

CYP2D6 (PA128) CYP2D6*1, CYP2D6*2

Evidence: -; PMID 12960748

CYP2D6 (PA128) CYP2D6*1, CYP2D6*10

Evidence: -; PMID 12960748

CYP2D6 (PA128) CYP2D6 poor metabolizer

Evidence: -; PMID 26514968

EPM2A (PA27832) rs1415744

Evidence: -; PMID 27092952

ABCB5 (PA24387) rs17143212

Evidence: -; PMID 25647612

CYP2D6 (PA128) rs3892097

Evidence: -; PMID 27695358

CYP3A43 (PA427) rs680055

Evidence: -; PMID 25150845

CYP2D6 (PA128) CYP2D6 haplotype

Evidence: -; PMID 25868121

CYP3A4 (PA130) CYP3A4*1, CYP3A4*22

Evidence: -; PMID 25868121

CYP3A4 (PA130) rs2242480

Evidence: -; PMID 23077486

- rs12970134

Evidence: -; PMID 22566560

CYP2D6 (PA128) CYP2D6*6

Evidence: -; PMID 27469576

CYP3A4 (PA130) rs2242480

Evidence: -; PMID 23077486

SOURCE RxNorm drug names 12 name rows

Drug Names / RxNorm

Normalized drug-name vocabulary rows, RxCUIs, and source abbreviations.

Name	RxCUI	Type	Source
Haloperidol	5093	SU	MTHSPL
HALOPERIDOL	5093	SU	MTHSPL
haloperidol	5093	SU	MTHSPL
HALOPERIDOL DECANOATE	26420	SU	MTHSPL
haloperidol decanoate	26420	SU	MTHSPL
haloperidol lactate	217483	SU	MTHSPL
HALOPERIDOL LACTATE	217483	SU	MTHSPL
Haloperidol lactate	217483	SU	MTHSPL
haloperidol	5093	IN	RXNORM
haloperidol decanoate	26420	PIN	RXNORM
Haldol	151839	BN	RXNORM
haloperidol lactate	217483	PIN	RXNORM

SOURCE SIDER side-effect resource 80 side-effect rows

Side Effects

SIDER side-effect terms mapped to the drug or same-CAS compound identity.

Side Effect	Drug Name	MedDRA Type	Concept ID
Abnormal behaviour	haloperidol	PT	C0233514
Acute hepatic failure	haloperidol	LLT	C0162557
Acute hepatic failure	haloperidol	PT	C0162557
Agitation	haloperidol	LLT	C0085631
Agitation	haloperidol	PT	C0085631
Agitation	haloperidol	PT	C0085631
Agranulocytosis	haloperidol	LLT	C0001824
Agranulocytosis	haloperidol	PT	C0001824
Akathisia	haloperidol	LLT	C0392156
Akathisia	haloperidol	PT	C0392156
Akinesia	haloperidol	LLT	C0085623
Akinesia	haloperidol	PT	C0085623
Alopecia	haloperidol	LLT	C0002170
Alopecia	haloperidol	PT	C0002170
Amenorrhoea	haloperidol	LLT	C0002453
Amenorrhoea	haloperidol	PT	C0002453
Anaemia	haloperidol	LLT	C0002871
Anaemia	haloperidol	PT	C0002871
Anaphylactic shock	haloperidol	LLT	C0002792
Anaphylactic shock	haloperidol	PT	C0002792
Angiopathy	haloperidol	LLT	C0042373
Angiopathy	haloperidol	PT	C0042373
Anorexia	haloperidol	LLT	C0003123
Anxiety	haloperidol	LLT	C0003467
Anxiety	haloperidol	PT	C0003467
Argininosuccinate synthetase deficiency	haloperidol	LLT	C0175683
Argininosuccinate synthetase deficiency	haloperidol	PT	C0175683
Blood and lymphatic system disorders	haloperidol	-	C0851353
Body temperature decreased	haloperidol	LLT	C0020672
Body temperature decreased	haloperidol	PT	C0020672
Body temperature increased	haloperidol	LLT	C0015967
Body temperature increased	haloperidol	PT	C0015967
Bradykinesia	haloperidol	LLT	C0233565
Bradykinesia	haloperidol	PT	C0233565
Breast discomfort	haloperidol	LLT	C0877338
Breast discomfort	haloperidol	PT	C0877338
Breast disorder	haloperidol	LLT	C0006145
Breast disorder	haloperidol	PT	C0006145
Breast engorgement	haloperidol	LLT	C0085688
Breast engorgement	haloperidol	PT	C0085688
Breast pain	haloperidol	LLT	C0024902
Breast pain	haloperidol	PT	C0024902
Bronchospasm	haloperidol	LLT	C0006266
Bronchospasm	haloperidol	PT	C0006266
Cardiac arrest	haloperidol	LLT	C0018790
Cardiac arrest	haloperidol	PT	C0018790
Cardiac disorder	haloperidol	LLT	C0018799
Cardiac disorder	haloperidol	PT	C0018799
Cataract	haloperidol	LLT	C0086543
Cataract	haloperidol	PT	C0086543
Catatonia	haloperidol	LLT	C0007398
Catatonia	haloperidol	PT	C0007398
Cholestasis	haloperidol	LLT	C0008370
Cholestasis	haloperidol	PT	C0008370
Cogwheel rigidity	haloperidol	LLT	C0151564
Cogwheel rigidity	haloperidol	PT	C0151564
Confusional state	haloperidol	LLT	C0009676
Confusional state	haloperidol	PT	C0009676
Connective tissue disorder	haloperidol	LLT	C0009782
Connective tissue disorder	haloperidol	PT	C0009782
Constipation	haloperidol	LLT	C0009806
Constipation	haloperidol	PT	C0009806
Convulsion	haloperidol	LLT	C0036572
Convulsion	haloperidol	PT	C0036572
Decreased appetite	haloperidol	PT	C0232462
Depression	haloperidol	LLT	C0011570
Depression	haloperidol	PT	C0011570
Dermatitis	haloperidol	PT	C0011603
Dermatitis exfoliative	haloperidol	LLT	C0011606
Dermatitis exfoliative	haloperidol	PT	C0011606
Diarrhoea	haloperidol	LLT	C0011991
Diarrhoea	haloperidol	PT	C0011991
Disturbance in sexual arousal	haloperidol	PT	C0855242
Disturbance in sexual arousal	haloperidol	PT	C0855242
Dizziness	haloperidol	LLT	C0012833
Dizziness	haloperidol	PT	C0012833
Drowsiness	haloperidol	LLT	C0013144
Drug withdrawal syndrome neonatal	haloperidol	LLT	C0027609
Drug withdrawal syndrome neonatal	haloperidol	PT	C0027609
Dry mouth	haloperidol	LLT	C0043352

SOURCE Rendered pharma page rows FAQPage JSON-LD

Frequently Asked Questions

Short answers generated only from the same visible source-linked rows on this page.

What is Haloperidol used for in pharmaceutical contexts?

Haloperidol (CAS 52-86-8) is rendered as a pharmaceutical compound from the matched source rows; no DailyMed product-name rows are present in this page query.

What are the known adverse events for Haloperidol?

Haloperidol has 2,675 DrugCentral/FAERS adverse event associations. Rendered reaction terms include Neuroleptic malignant syndrome, Extrapyramidal disorder, Intentional self-injury, Akathisia, Dystonia. Signal rows are source-linked records and should not be read as incidence rates or causality conclusions.

Is Haloperidol also used in cosmetics?

No same-CAS cosmetics profile is rendered from the ingredients-table cross-reference for Haloperidol.

What clinical phase is Haloperidol in?

Haloperidol is rendered with ChEMBL max phase 4 (approved).

What bioactivity targets are documented for Haloperidol?

Haloperidol has 93 bioactivity rows in this page query. Rendered target entries include Calmodulin, 5-hydroxytryptamine receptor 5A, 5-hydroxytryptamine receptor 1F, 5-hydroxytryptamine receptor 1E, Beta-2 adrenergic receptor.