Haloprogin

Summary

Haloprogin (CHEMBL1289) is an approved small molecule (ATC D01AE11).

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: D01AE11
• Chemistry: 361.4 Da · C9H4Cl3IO

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1289
Name	Haloprogin
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	3561
ATC	D01AE11
Molecular formula	C9H4Cl3IO
Molecular weight	361.4
InChIKey	CTETYYAZBPJBHE-UHFFFAOYSA-N

SMILES: C1=C(C(=CC(=C1Cl)Cl)Cl)OCC#CI

IUPAC name: 1,2,4-trichloro-5-(3-iodoprop-2-ynoxy)benzene

Also known as: Haloprogin, Haloprogina, Haloprogine, Halotex, M-1028, M-1028 (MEIJI), Mycanden, NSC-100071, SID50125846, HALOPROGIN, SID144206294, SID225144320

Patent coverage: 2,309 distinct patent families (8,799 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 8,798 (100%) of the total. 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: 21 (assay-derived). Sample: Nuclear receptor ROR-gamma, 4’-phosphopantetheinyl transferase ffp, Alpha-2A adrenergic receptor, Alpha-2C adrenergic receptor, Alpha-2B adrenergic receptor, D(1A) dopamine receptor, Sodium-dependent noradrenaline transporter, 5-hydroxytryptamine receptor 2A, 5-hydroxytryptamine receptor 2C, Adenosine receptor A1.

Bioactivity

ChEMBL activities: 38 potent at pChembl ≥ 5 of 42 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
ADORA3	6.9	Ki	126	nM	CHEMBL_ACT_7645133
DRD3	6.78	Ki	166	nM	CHEMBL_ACT_7645215
ADORA3	6.65	IC50	223	nM	CHEMBL_ACT_7645132
ADRA2B	6.6	Ki	251	nM	CHEMBL_ACT_7645145
DRD1	6.55	Ki	282	nM	CHEMBL_ACT_7645211
SLC6A4	6.37	Ki	431	nM	CHEMBL_ACT_7647344
ADRA2A	6.34	Ki	458	nM	CHEMBL_ACT_7645143
OPRK1	6.34	Ki	459	nM	CHEMBL_ACT_7647272
DRD3	6.31	IC50	488	nM	CHEMBL_ACT_7645214
TACR2	6.31	Ki	491	nM	CHEMBL_ACT_7647354
GALE	6.3	IC50	500	nM	CHEMBL_ACT_1809343
ADRA2B	6.26	IC50	551	nM	CHEMBL_ACT_7645144
DRD1	6.25	IC50	563	nM	CHEMBL_ACT_7645210
ADRA2C	6.23	Ki	588	nM	CHEMBL_ACT_7645147
HTR2A	6.16	Ki	692	nM	CHEMBL_ACT_7647332
SLC6A4	6.09	IC50	811	nM	CHEMBL_ACT_7647343
ADORA3	6.02	AC50	945.9	nM	CHEMBL_ACT_25198751
DRD3	5.94	AC50	1159	nM	CHEMBL_ACT_25194562
OPRK1	5.94	IC50	1147	nM	CHEMBL_ACT_7647271
ADRA2A	5.91	IC50	1222	nM	CHEMBL_ACT_7645142
HTR2C	5.87	Ki	1363	nM	CHEMBL_ACT_7647336
TACR2	5.83	IC50	1474	nM	CHEMBL_ACT_7647353
SLC6A3	5.8	Ki	1565	nM	CHEMBL_ACT_7645219
HTR6	5.73	Ki	1862	nM	CHEMBL_ACT_7647342
SLC6A3	5.71	IC50	1969	nM	CHEMBL_ACT_7645218
HTR2A	5.62	IC50	2421	nM	CHEMBL_ACT_7647331
DRD1	5.6	AC50	2503	nM	CHEMBL_ACT_25115250
HTR2C	5.58	IC50	2602	nM	CHEMBL_ACT_7647335
SLC6A2	5.56	IC50	2770	nM	CHEMBL_ACT_7645154
SLC6A2	5.56	Ki	2747	nM	CHEMBL_ACT_7645155

Target pathways

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

Indications & clinical

Indications

0 indications (0 at ChEMBL trial phase 4).

Clinical trials

Total trials: 0.

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

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