Pinacidil Anhydrous

Summary

Pinacidil Anhydrous (CHEMBL1159) is an approved small molecule targeting KCNJ8 and KCNJ11.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• Targets: 2 (KCNJ8, KCNJ11)
• Chemistry: 245.32 Da · C13H19N5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1159
Name	Pinacidil Anhydrous
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	4826
Molecular formula	C13H19N5
Molecular weight	245.32
InChIKey	IVVNZDGDKPTYHK-UHFFFAOYSA-N

SMILES: CC(C(C)(C)C)N=C(NC#N)NC1=CC=NC=C1

IUPAC name: 1-cyano-2-(3,3-dimethylbutan-2-yl)-3-pyridin-4-ylguanidine

Also known as: (r,s)-pinacidil, P-1134, Pinacidil anhydrous, S-1230, pinacidil, Pinacidil, (+/-)-pinacidil, (+/-)-Pinacidil, SID11532877, SID26749106, SID50104869, SID56463565

Parent form; salt/anhydrous children: CHEMBL1200338

Patent coverage: 1,756 distinct patent families (6,303 SureChEMBL compound mentions), from 6 matched compound structure(s). One matched structure accounts for 6,141 (97%) 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

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
KCNJ8	Kir6.1	Agonist		0%	Q15842
KCNJ11	Kir6.2	Agonist		0.1%	Q14654

Broader ChEMBL bioactivity targets: 10 (assay-derived). Sample: Prelamin-A/C, RecQ-like DNA helicase BLM, Peripheral myelin protein 22, ATP-binding cassette sub-family C member 9, Beta-lactamase, Sulfonylurea receptor 2, Kir6.2, Alpha-galactosidase A, Cytochrome P450 3A4, Aldehyde dehydrogenase 1A1, Neuropeptide S receptor.

Bioactivity

ChEMBL activities: 10 potent at pChembl ≥ 5 of 12 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
ABCC9	6.5	Ki	320	nM	CHEMBL_ACT_478143
P00811	6.45	Potency	354.8	nM	CHEMBL_ACT_4683908
LMNA	5.9	Potency	1259	nM	CHEMBL_ACT_3655701
GLA	5.5	Potency	3162	nM	CHEMBL_ACT_4861136
CYP3A4	5.5	Potency	3162	nM	CHEMBL_ACT_4997868
CYP3A4	5.5	Potency	3162	nM	CHEMBL_ACT_5066577
ABCC9	5.45	EC50	3540	nM	CHEMBL_ACT_2395828
BLM	5.45	Potency	3548	nM	CHEMBL_ACT_4753991
BLM	5.45	Potency	3548	nM	CHEMBL_ACT_4886086
NPSR1	5.3	Potency	5012	nM	CHEMBL_ACT_4893433

Target pathways

Aggregated over 2 target gene(s): KCNJ8, KCNJ11.

Top Reactome pathways

17 total, by targets touching each:

Pathway	Targets	Genes
Neuronal System	2	KCNJ11, KCNJ8
ATP sensitive Potassium channels	2	KCNJ11, KCNJ8
Inwardly rectifying K+ channels	2	KCNJ11, KCNJ8
Potassium Channels	2	KCNJ11, KCNJ8
Metabolism	1	KCNJ11
Integration of energy metabolism	1	KCNJ11
Disease	1	KCNJ11
Transport of small molecules	1	KCNJ11
ABC-family protein mediated transport	1	KCNJ11
Muscle contraction	1	KCNJ11
Regulation of insulin secretion	1	KCNJ11
Cardiac conduction	1	KCNJ11
Ion homeostasis	1	KCNJ11
ABC transporter disorders	1	KCNJ11
Disorders of transmembrane transporters	1	KCNJ11
Defective ABCC9 causes CMD10, ATFB12 and Cantu syndrome	1	KCNJ11
Defective ABCC8 can cause hypo- and hyper-glycemias	1	KCNJ11

Dominant GO biological processes

GO term	Targets
response to hypoxia	2
response to ischemia	2
ventricular cardiac muscle tissue development	2
potassium ion transport	2
apoptotic process	2
determination of adult lifespan	2
response to xenobiotic stimulus	2
response to ATP	2
regulation of monoatomic ion transmembrane transport	2
CAMKK-AMPK signaling cascade	2
potassium ion transmembrane transport	2
obsolete inorganic cation transmembrane transport	2
response to resveratrol	2
potassium ion import across plasma membrane	2
action potential	2

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 PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

7 molecules share ≥1 primary target. Top 7 by shared-target count:

Molecule	Source	Status	Shared targets
glyburide	ChEMBL + PubChem	Phase 4 (approved)	KCNJ11, KCNJ8
CROMAKALIM	ChEMBL	Phase 2	KCNJ11, KCNJ8
DIAZOXIDE	ChEMBL + PubChem	Phase 4 (approved)	KCNJ11
PROPAFENONE	ChEMBL + PubChem	Phase 4 (approved)	KCNJ11
CLAMIKALANT	ChEMBL	Phase 2	KCNJ11
TIFENAZOXIDE	ChEMBL	Phase 2	KCNJ11
Berberine Chloride	PubChem	Approved	KCNJ11