Inamrinone

drug
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Also known as AmcoralAmrinonaAmrinoneC01CE01CartonicCordemcuraNSC-759805VesistolWIN 40680WIN-40680WincoramSID11112811SID11533005SID26750001SID26757798SID56424028SID124882647SID170465367SID144205663

Summary

Inamrinone (CHEMBL12856) is an approved small-molecule EC 3.1.4.* (phosphoric diester hydrolase) inhibitor (ATC C01CE01) targeting PDE3A and PDE3B; indicated across 1 condition including cardiovascular disorder.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: C01CE01
  • Targets: 2 (PDE3A, PDE3B)
  • Indications: 1 condition
  • Chemistry: 187.2 Da · C10H9N3O

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL12856
NameInamrinone
TypeSmall molecule
Max phase4
FDA approvedno
PubChem CID3698
ChEBICHEBI:2686
ATCC01CE01
Molecular formulaC10H9N3O
Molecular weight187.2
InChIKeyRNLQIBCLLYYYFJ-UHFFFAOYSA-N

SMILES: C1=CN=CC=C1C2=CNC(=O)C(=C2)N

IUPAC name: 3-amino-5-pyridin-4-yl-1H-pyridin-2-one

ChEBI definition: A 3,4’-bipyridine substituted at positions 5 and 6 by an amino group and a keto function respectively. A pyridine phosphodiesterase 3 inhibitor, it is a drug that may improve the prognosis in patients with congestive heart failure.

Pharmacological roles (ChEBI): EC 3.1.4.* (phosphoric diester hydrolase) inhibitor, cardiovascular drug.

Also known as: Amcoral, Amrinona, Amrinone, C01CE01, Cartonic, Cordemcura, Inamrinone, NSC-759805, Vesistol, WIN 40680, WIN-40680, Wincoram

Parent form; salt/anhydrous children: CHEMBL2096642

Patent coverage: 2,680 distinct patent families (9,690 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 9,689 (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

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

GeneTargetActionpAffinityCancer dependencyUniProt
PDE3Aphosphodiesterase 3AInhibition4.80.1%Q14432
PDE3Bphosphodiesterase 3BInhibition4.510.2%Q13370

Broader ChEMBL bioactivity targets: 36 (assay-derived). Sample: Microtubule-associated protein tau, Lysine-specific demethylase 4E, Nuclear receptor ROR-gamma, Survival motor neuron protein, Fructose-bisphosphate aldolase, Prelamin-A/C, ATP-dependent DNA helicase Q1, RecQ-like DNA helicase BLM, 4’-phosphopantetheinyl transferase ffp, Ferritin light chain, 15-hydroxyprostaglandin dehydrogenase [NAD(+)], Alpha-2B adrenergic receptor, Thyroid hormone receptor beta, Beta-lactamase, Menin/Histone-lysine N-methyltransferase MLL, Phosphodiesterase 4, Phosphodiesterase 3, Phosphodiesterase; PDE3 & PDE4, cGMP-inhibited 3’,5’-cyclic phosphodiesterase 3A, Alpha-galactosidase A.

Bioactivity

ChEMBL activities: 29 potent at pChembl ≥ 5 of 80 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
P027916.55Potency281.8nMCHEMBL_ACT_4491761
LMNA6.5Potency316.2nMCHEMBL_ACT_3660379
HTT6.3Potency501.2nMCHEMBL_ACT_3749757
KDM4E5.95Potency1122nMCHEMBL_ACT_3733314
HSD17B105.9Potency1259nMCHEMBL_ACT_4829782
GLA5.9Potency1259nMCHEMBL_ACT_4849183
MAPT5.85Potency1412nMCHEMBL_ACT_4061090
A8B2U25.75Potency1774nMCHEMBL_ACT_4611837
MAPT5.7Potency1995nMCHEMBL_ACT_4525518
ADRA2B5.64AC502300nMCHEMBL_ACT_25144361
CYP3A45.5Potency3162nMCHEMBL_ACT_5006308
CYP3A45.5Potency3162nMCHEMBL_ACT_5074815
CYP3A45.5AC503162nMCHEMBL_ACT_6053661
MAPT5.45Potency3548nMCHEMBL_ACT_4044933
A8B2U25.45Potency3540nMCHEMBL_ACT_4600411
HIF1A5.4Potency3981nMCHEMBL_ACT_4128841
HIF1A5.4Potency3981nMCHEMBL_ACT_4520663
A8B2U25.4Potency3972nMCHEMBL_ACT_4608785
MAPT5.35Potency4467nMCHEMBL_ACT_4505683
PDE4A5.32IC504800nMCHEMBL_ACT_172836
MAPT5.3Potency5012nMCHEMBL_ACT_3971813
CYP2C195.3Potency5012nMCHEMBL_ACT_4015454
CYP2C195.3AC505012nMCHEMBL_ACT_6056783
Q9F4F75.25Potency5623nMCHEMBL_ACT_4399453
Q9F4F75.2Potency6310nMCHEMBL_ACT_4374675
MEN15.2Potency6310nMCHEMBL_ACT_4592405
MAPT5.05Potency8912nMCHEMBL_ACT_3904894
HSD17B105Potency10000nMCHEMBL_ACT_3712667
MAPT5Potency10000nMCHEMBL_ACT_3953035

Target pathways

Aggregated over 2 target gene(s): PDE3A, PDE3B.

Top Reactome pathways

2 total, by targets touching each:

PathwayTargetsGenes
G alpha (s) signalling events2PDE3A, PDE3B
PDE3B signalling1PDE3B

Dominant GO biological processes

GO termTargets
G protein-coupled receptor signaling pathway2
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathway2
negative regulation of cAMP/PKA signal transduction2
signal transduction2
oocyte maturation1
lipid metabolic process1
response to xenobiotic stimulus1
regulation of meiotic nuclear division1
negative regulation of apoptotic process1
negative regulation of vascular permeability1
positive regulation of vascular permeability1
positive regulation of oocyte development1
regulation of ribonuclease activity1
cellular response to cGMP1
cellular response to transforming growth factor beta stimulus1

Indications & clinical

Indications

1 approved indication. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

IndicationPhaseMONDOEFO
cardiovascular disorder4MONDO:0004995EFO:0000319

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.

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.

200 molecules share ≥1 primary target. Top 100 by shared-target count:

MoleculeSourceStatusShared targets
ANAGRELIDEChEMBL + PubChemPhase 4 (approved)PDE3A, PDE3B
LOSARTANChEMBL + PubChemPhase 4 (approved)PDE3A, PDE3B
SILDENAFILChEMBL + PubChemPhase 4 (approved)PDE3A, PDE3B
VARDENAFILChEMBL + PubChemPhase 4 (approved)PDE3A, PDE3B
CILOSTAZOLChEMBLPhase 4 (approved)PDE3A, PDE3B
CRISABOROLEChEMBLPhase 4 (approved)PDE3A, PDE3B
DIPYRIDAMOLEChEMBLPhase 4 (approved)PDE3A, PDE3B
ENOXIMONEChEMBLPhase 4 (approved)PDE3A, PDE3B
IBUDILASTChEMBLPhase 4 (approved)PDE3A, PDE3B
MILRINONEChEMBLPhase 4 (approved)PDE3A, PDE3B
LEVOSIMENDANChEMBLPhase 3PDE3A, PDE3B
PAPAVERINEChEMBLPhase 3PDE3A, PDE3B
ADIBENDANChEMBLPhase 2PDE3A, PDE3B
BEMARINONEChEMBLPhase 2PDE3A, PDE3B
BEMORADANChEMBLPhase 2PDE3A, PDE3B
CC-115ChEMBLPhase 2PDE3A, PDE3B
CILOSTAMIDEChEMBLPhase 2PDE3A, PDE3B
ETAZOLATEChEMBLPhase 2PDE3A, PDE3B
IMAZODANChEMBLPhase 2PDE3A, PDE3B
INDOLIDANChEMBLPhase 2PDE3A, PDE3B
ISOMAZOLEChEMBLPhase 2PDE3A, PDE3B
LIXAZINONEChEMBLPhase 2PDE3A, PDE3B
MEDORINONEChEMBLPhase 2PDE3A, PDE3B
MERIBENDANChEMBLPhase 2PDE3A, PDE3B
ORISMILASTChEMBLPhase 2PDE3A, PDE3B
OXAGRELATEChEMBLPhase 2PDE3A, PDE3B
PIMOBENDANChEMBLPhase 2PDE3A, PDE3B
PIROXIMONEChEMBLPhase 2PDE3A, PDE3B
QUAZINONEChEMBLPhase 2PDE3A, PDE3B
SIMENDANChEMBLPhase 2PDE3A, PDE3B
SULMAZOLEChEMBLPhase 2PDE3A, PDE3B
VESNARINONEChEMBLPhase 2PDE3A, PDE3B
ZARDAVERINEChEMBLPhase 2PDE3A, PDE3B
TadalafilPubChemApprovedPDE3A, PDE3B
CLOFARABINEChEMBL + PubChemPhase 4 (approved)PDE3A
IDELALISIBChEMBL + PubChemPhase 4 (approved)PDE3A
TAFAMIDISChEMBL + PubChemPhase 4 (approved)PDE3A
TAVABOROLEChEMBL + PubChemPhase 4 (approved)PDE3A
ACARBOSEChEMBLPhase 4 (approved)PDE3A
ADENOSINEChEMBLPhase 4 (approved)PDE3A
ALECTINIBChEMBLPhase 4 (approved)PDE3A
ALENDRONIC ACIDChEMBLPhase 4 (approved)PDE3A
AMINOGLUTETHIMIDEChEMBLPhase 4 (approved)PDE3A
AMLEXANOXChEMBLPhase 4 (approved)PDE3A
ANTAZOLINEChEMBLPhase 4 (approved)PDE3A
ARIPIPRAZOLEChEMBLPhase 4 (approved)PDE3A
BENAZEPRILChEMBLPhase 4 (approved)PDE3A
BENZBROMARONEChEMBLPhase 4 (approved)PDE3A
BITHIONOLChEMBLPhase 4 (approved)PDE3A
CABOZANTINIBChEMBLPhase 4 (approved)PDE3A
CALCITRIOLChEMBLPhase 4 (approved)PDE3A
CANDESARTAN CILEXETILChEMBLPhase 4 (approved)PDE3A
CANNABIDIOLChEMBLPhase 4 (approved)PDE3A
CEFOPERAZONEChEMBLPhase 4 (approved)PDE3A
CHLORHEXIDINEChEMBLPhase 4 (approved)PDE3A
CHLOROQUINEChEMBLPhase 4 (approved)PDE3A
CHOLIC ACIDChEMBLPhase 4 (approved)PDE3A
CINNARIZINEChEMBLPhase 4 (approved)PDE3A
CLADRIBINEChEMBLPhase 4 (approved)PDE3A
CODEINEChEMBLPhase 4 (approved)PDE3A
DEOXYCHOLIC ACIDChEMBLPhase 4 (approved)PDE3A
DEQUALINIUMChEMBLPhase 4 (approved)PDE3A
DISOPYRAMIDEChEMBLPhase 4 (approved)PDE3A
DUVELISIBChEMBLPhase 4 (approved)PDE3A
EFAVIRENZChEMBLPhase 4 (approved)PDE3A
ENCORAFENIBChEMBLPhase 4 (approved)PDE3A
ESTRADIOL CYPIONATEChEMBLPhase 4 (approved)PDE3A
ESTRADIOL VALERATEChEMBLPhase 4 (approved)PDE3A
ETHINYL ESTRADIOLChEMBLPhase 4 (approved)PDE3A
FEXOFENADINEChEMBLPhase 4 (approved)PDE3A
GEMCITABINEChEMBLPhase 4 (approved)PDE3A
GRISEOFULVINChEMBLPhase 4 (approved)PDE3A
HEXACHLOROPHENEChEMBLPhase 4 (approved)PDE3A
HYDROXOCOBALAMINChEMBLPhase 4 (approved)PDE3A
HYDROXYPROGESTERONE CAPROATEChEMBLPhase 4 (approved)PDE3A
IBANDRONIC ACIDChEMBLPhase 4 (approved)PDE3A
IDEBENONEChEMBLPhase 4 (approved)PDE3A
IFOSFAMIDEChEMBLPhase 4 (approved)PDE3A
ILOPERIDONEChEMBLPhase 4 (approved)PDE3A
INDOCYANINE GREEN ACID FORMChEMBLPhase 4 (approved)PDE3A
IRBESARTANChEMBLPhase 4 (approved)PDE3A
ISOPROTERENOLChEMBLPhase 4 (approved)PDE3A
ISRADIPINEChEMBLPhase 4 (approved)PDE3A
LAMIVUDINEChEMBLPhase 4 (approved)PDE3A
LAMOTRIGINEChEMBLPhase 4 (approved)PDE3A
MASOPROCOLChEMBLPhase 4 (approved)PDE3A
MECLIZINEChEMBLPhase 4 (approved)PDE3A
METHICILLINChEMBLPhase 4 (approved)PDE3A
MIZOLASTINEChEMBLPhase 4 (approved)PDE3A
MOEXIPRILChEMBLPhase 4 (approved)PDE3A
MOFEZOLACChEMBLPhase 4 (approved)PDE3A
MONTELUKASTChEMBLPhase 4 (approved)PDE3A
MYCOPHENOLATE MOFETILChEMBLPhase 4 (approved)PDE3A
NEVIRAPINEChEMBLPhase 4 (approved)PDE3A
NISOLDIPINEChEMBLPhase 4 (approved)PDE3A
NITROFURAZONEChEMBLPhase 4 (approved)PDE3A
NORETHYNODRELChEMBLPhase 4 (approved)PDE3A
OLAPARIBChEMBLPhase 4 (approved)PDE3A
OLMESARTAN MEDOXOMILChEMBLPhase 4 (approved)PDE3A
PAMIDRONIC ACIDChEMBLPhase 4 (approved)PDE3A