Bromperidol

Summary

Bromperidol (CHEMBL28218) is an approved small molecule (ATC N05AD06); indicated across 5 conditions including psychotic disorder and anxiety.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N05AD06
• Indications: 5 conditions
• Clinical trials: 2
• Chemistry: 420.3 Da · C21H23BrFNO2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL28218
Name	Bromperidol
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	2448
ATC	N05AD06
Molecular formula	C21H23BrFNO2
Molecular weight	420.3
InChIKey	RKLNONIVDFXQRX-UHFFFAOYSA-N

SMILES: C1CN(CCC1(C2=CC=C(C=C2)Br)O)CCCC(=O)C3=CC=C(C=C3)F

IUPAC name: 4-[4-(4-bromophenyl)-4-hydroxypiperidin-1-yl]-1-(4-fluorophenyl)butan-1-one

Also known as: Bromperidol, NSC-759275, R 11,333, R-11333, SID11112600, SID56463221, BROMPERIDOL, SID144204116, SID170465873, bromperidol

Patent coverage: 1,084 distinct patent families (4,331 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 25 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Alpha-2C adrenergic receptor, Alpha-2B adrenergic receptor, Beta-lactamase, 5-hydroxytryptamine receptor 1A, Muscarinic acetylcholine receptor M1, D(2) dopamine receptor, Sodium-dependent noradrenaline transporter, 5-hydroxytryptamine receptor 2A.

Bioactivity

ChEMBL activities: 24 potent at pChembl ≥ 5 of 28 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
DRD2	7.66	AC50	22	nM	CHEMBL_ACT_25140901
DRD3	7.39	AC50	41	nM	CHEMBL_ACT_25194086
KCNH2	6.64	AC50	230	nM	CHEMBL_ACT_25118674
P9WFK7	6.62	Ki	240	nM	CHEMBL_ACT_24705488
ADRA1A	6.55	AC50	280	nM	CHEMBL_ACT_25218477
P9WFK7	6.28	IC50	520	nM	CHEMBL_ACT_24705424
HTR1A	5.92	AC50	1200	nM	CHEMBL_ACT_25216412
HTR2A	5.75	AC50	1800	nM	CHEMBL_ACT_25225688
OPRM1	5.7	AC50	2000	nM	CHEMBL_ACT_25147257
SLC6A4	5.57	AC50	2700	nM	CHEMBL_ACT_25150882
NR1I2	5.43	AC50	3700	nM	CHEMBL_ACT_25224614
CYP2D6	5.4	Potency	3981	nM	CHEMBL_ACT_5010613
CYP2D6	5.4	AC50	3981	nM	CHEMBL_ACT_6041863
SLC6A2	5.31	AC50	4900	nM	CHEMBL_ACT_25145553
CYP1A2	5.3	AC50	5012	nM	CHEMBL_ACT_6016186
SLC6A3	5.19	AC50	6500	nM	CHEMBL_ACT_25124509
GHSR	5.16	AC50	6900	nM	CHEMBL_ACT_25173294
HTR2B	5.14	AC50	7300	nM	CHEMBL_ACT_25228060
ADRA2C	5.1	AC50	8000	nM	CHEMBL_ACT_25148450
P00811	5.1	Potency	7943	nM	CHEMBL_ACT_4673757
HRH1	5.01	AC50	9800	nM	CHEMBL_ACT_25213083
OPRK1	5	AC50	10000	nM	CHEMBL_ACT_25129946
CYP3A4	5	Potency	10000	nM	CHEMBL_ACT_5006364
CYP3A4	5	Potency	10000	nM	CHEMBL_ACT_5074871

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

5 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
psychotic disorder	4	MONDO:0005485	EFO:0005407
anxiety	3	MONDO:0011918	EFO:0005230
dementia	3	MONDO:0001627	HP:0000726
depressive disorder	3	MONDO:0002050	MONDO:0002050

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 2.

Phase distribution

Phase	Trials
PHASE4	1
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02307396	PHASE4	COMPLETED	Evaluation of the Necessity of Long-term Pharmacological Treatment With Antipsychotics in Schizophrenic Patients
NCT02374567	PHASE3	TERMINATED	Pharmacovigilance in Gerontopsychiatric Patients

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 1 clinical and 1 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).