Chlorproguanil

Summary

Chlorproguanil (CHEMBL1213553) is a phase-3 clinical-stage small molecule; indicated across 4 conditions including malaria and plasmodium falciparum malaria.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 4 conditions
• Clinical trials: 15
• Chemistry: 288.17 Da · C11H15Cl2N5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1213553
Name	Chlorproguanil
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	9571037
Molecular formula	C11H15Cl2N5
Molecular weight	288.17
InChIKey	ISZNZKHCRKXXAU-UHFFFAOYSA-N

SMILES: CC(C)N=C(N)/N=C(\N)/NC1=CC(=C(C=C1)Cl)Cl

IUPAC name: (1E)-1-[amino-(3,4-dichloroanilino)methylidene]-2-propan-2-ylguanidine

Also known as: Chlorproguanil, Clorproguanil, CHLORPROGUANIL, Proguanil, chlorproguanil

Parent form; salt/anhydrous children: CHEMBL2107534

Patent coverage: 800 distinct patent families (2,526 SureChEMBL compound mentions), from 4 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: 15 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Alpha-2C adrenergic receptor, Alpha-2B adrenergic receptor, D(1A) dopamine receptor, Muscarinic acetylcholine receptor M2, 5-hydroxytryptamine receptor 1A, Sodium-dependent noradrenaline transporter, 5-hydroxytryptamine receptor 2A, 5-hydroxytryptamine receptor 2C, Sodium-dependent serotonin transporter, Alpha-1A adrenergic receptor, Mu-type opioid receptor, Sodium-dependent dopamine transporter, Voltage-gated inwardly rectifying potassium channel KCNH2.

Bioactivity

ChEMBL activities: 12 potent at pChembl ≥ 5 of 16 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
DRD1	5.75	AC50	1770	nM	CHEMBL_ACT_25115049
SLC6A3	5.73	AC50	1860	nM	CHEMBL_ACT_25124798
KCNH2	5.58	AC50	2600	nM	CHEMBL_ACT_25117351
ADRA1A	5.56	AC50	2740	nM	CHEMBL_ACT_25234630
SLC6A2	5.54	AC50	2890	nM	CHEMBL_ACT_25145839
HTR2A	5.44	AC50	3600	nM	CHEMBL_ACT_25224860
HTR1A	5.42	AC50	3820	nM	CHEMBL_ACT_25164863
ADRA2A	5.25	AC50	5590	nM	CHEMBL_ACT_25156268
SLC6A4	5.24	AC50	5810	nM	CHEMBL_ACT_25151166
HTR2C	5.1	AC50	7900	nM	CHEMBL_ACT_25131476
ADRA2C	5.05	AC50	8900	nM	CHEMBL_ACT_25147533
ADRA2B	5	AC50	10000	nM	CHEMBL_ACT_25143368

Target pathways

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

Indications & clinical

Indications

3 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
malaria	3	MONDO:0005136	EFO:0001068
Plasmodium falciparum malaria	3	MONDO:0005920	EFO:0007444
Plasmodium vivax malaria	3	MONDO:0005921	EFO:0007445

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

Clinical trials

Total trials: 15.

Phase distribution

Phase	Trials
PHASE4	4
PHASE1	3
Not specified	3
PHASE2/PHASE3	2
PHASE3	1
PHASE2	1
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00421473	PHASE4	COMPLETED	Drug Interaction Study Between Atovaquone and Antiretroviral Agents in HIV-1 Infected Patients
NCT00451139	PHASE4	COMPLETED	Ototoxicity of Artemether / Lumefantrine (Coartem) and Other Antimalarials
NCT02564471	PHASE4	COMPLETED	Effect of Antimalarial Drugs to Rabies Vaccine for Post-exposure Prophylaxis.
NCT03178643	PHASE4	COMPLETED	Enhancing Preventive Therapy of Malaria In Children With Sickle Cell Anemia in East Africa (EPiTOMISE)
NCT00084227	PHASE2/PHASE3	COMPLETED	Azithromycin Plus Chloroquine Versus Atovaquone-Proguanil For The Treatment Of Uncomplicated Plasmodium Falciparum Malaria In South America
NCT00158574	PHASE2/PHASE3	COMPLETED	Kilimanjaro IPTi Drug Options Trial
NCT00361114	PHASE3	TERMINATED	IPT and Efficacy of Sulphadoxine/Pyrimethamine and Chlorproguanil/Dapsone in 6-59 Month Old Children With Malaria.
NCT00984256	PHASE2	COMPLETED	Weekly Dosing of Malarone ® for Prevention of Malaria
NCT01319448	PHASE1/PHASE2	COMPLETED	Intermittent Preventive Treatment for Malaria in Patient With Sickle Cell Disease
NCT01456546	PHASE1	COMPLETED	Impact of CYP2C19*17 on the Pharmacokinetics of Proguanil and Clopidogrel
NCT04568772	PHASE1	COMPLETED	Study to Evaluate the Influence of Tegoprazan on the Pharmacokinetics of Proguanil in Healthy Volunteers
NCT06294912	PHASE1	COMPLETED	A Study to Evaluate Antimalarial Activity and Safety of MK-7602 in Healthy Adults (MK-7602-003)
NCT02080026	Not specified	COMPLETED	Target Antigens Induced by Plasmodium Falciparum Sporozoite Immunization Under Chemoprophylaxis
NCT02098590	Not specified	COMPLETED	Chemoprophylaxis and Plasmodium Falciparum NF54 Sporozoite Immunization Challenged by Heterologous Infection
NCT03454048	Not specified	COMPLETED	Controlled Human Malaria Infection Model for Evaluation of Transmission-blocking Interventions - Study 2

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 4 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).