ARRY-797

drug
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Also known as ARRY-371797

Summary

Arry-797 (CHEMBL1088750) is a phase-3 clinical-stage small molecule targeting MAPK14; indicated across 5 conditions including dilated cardiomyopathy and ankylosing spondylitis.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Targets: 1 (MAPK14)
  • Indications: 5 conditions
  • Clinical trials: 9
  • Chemistry: 416.5 Da · C22H26F2N4O2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL1088750
NameARRY-797
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID46883775
Molecular formulaC22H26F2N4O2
Molecular weight416.5
InChIKeyIFGWYHGYNVGVRB-UHFFFAOYSA-N

SMILES: CC(C)CN1C2=CC(=C(C=C2C=N1)OC3=C(C=C(C=C3)F)F)C(=O)NCCN(C)C

IUPAC name: 5-(2,4-difluorophenoxy)-N-[2-(dimethylamino)ethyl]-1-(2-methylpropyl)indazole-6-carboxamide

Also known as: ARRY-371797, Arry-797, ARRY-797

Patent coverage: 202 distinct patent families (641 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 457 (71%) 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
MAPK14mitogen-activated protein kinase 14Inhibition8.359%Q16539

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Mitogen-activated protein kinase 14.

Bioactivity

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

TargetpChemblTypeValueUnitActivity ID
MAPK148.35IC504.5nMCHEMBL_ACT_3260866

Target pathways

Aggregated over 1 target gene(s): MAPK14.

Top Reactome pathways

78 total, by targets touching each:

PathwayTargetsGenes
Hemostasis1MAPK14
Developmental Biology1MAPK14
Cytokine Signaling in Immune system1MAPK14
Mitochondrial biogenesis1MAPK14
Signal Transduction1MAPK14
Disease1MAPK14
Toll Like Receptor 4 (TLR4) Cascade1MAPK14
MyD88:MAL(TIRAP) cascade initiated on plasma membrane1MAPK14
MyD88-independent TLR4 cascade1MAPK14
Signaling by NTRKs1MAPK14
Signalling to RAS1MAPK14
Toll Like Receptor 9 (TLR9) Cascade1MAPK14
Toll Like Receptor 10 (TLR10) Cascade1MAPK14
Toll Like Receptor 3 (TLR3) Cascade1MAPK14
Toll Like Receptor 5 (TLR5) Cascade1MAPK14
Toll Like Receptor TLR1:TLR2 Cascade1MAPK14
Toll Like Receptor 7/8 (TLR7/8) Cascade1MAPK14
Toll Like Receptor TLR6:TLR2 Cascade1MAPK14
Innate Immune System1MAPK14
Immune System1MAPK14
NOD1/2 Signaling Pathway1MAPK14
Nucleotide-binding domain, leucine rich repeat containing receptor (NLR) signaling pathways1MAPK14
Toll-like Receptor Cascades1MAPK14
p38MAPK events1MAPK14
Toll Like Receptor 2 (TLR2) Cascade1MAPK14
Organelle biogenesis and maintenance1MAPK14
Signaling by NTRK1 (TRKA)1MAPK14
Signalling to ERKs1MAPK14
Signaling by VEGF1MAPK14
Signaling by Rho GTPases1MAPK14

Dominant GO biological processes

GO termTargets
DNA damage checkpoint signaling1
MAPK cascade1
cell morphogenesis1
cartilage condensation1
angiogenesis1
osteoblast differentiation1
placenta development1
response to dietary excess1
chondrocyte differentiation1
negative regulation of inflammatory response to antigenic stimulus1
glucose metabolic process1
regulation of transcription by RNA polymerase II1
transcription by RNA polymerase II1
apoptotic process1
chemotaxis1

Indications & clinical

Indications

5 indications (0 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).

IndicationTrial phaseMONDOEFO
dilated cardiomyopathy3MONDO:0005021EFO:0000407
ankylosing spondylitis2MONDO:0005306EFO:0003898
osteoarthritis, knee2MONDO:0005416EFO:0004616
rheumatoid arthritis1MONDO:0008383EFO:0000685

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

Clinical trials

Total trials: 9.

Phase distribution

PhaseTrials
PHASE26
PHASE12
PHASE31

Top trials by phase / activity

NCTPhaseStatusTitle
NCT03439514PHASE3TERMINATEDA Study of ARRY-371797 (PF-07265803) in Patients With Symptomatic Dilated Cardiomyopathy Due to a Lamin A/C Gene Mutation
NCT00542035PHASE2COMPLETEDA Study of ARRY-371797 in Subjects Undergoing Third Molar Extraction
NCT00663767PHASE2COMPLETEDA Study of ARRY-371797 in Subjects Undergoing Third Molar Extraction
NCT00811499PHASE2TERMINATEDA Study of ARRY-371797 in Patients With Active Ankylosing Spondylitis
NCT01366014PHASE2COMPLETEDA Study of ARRY-371797 in Patients With Osteoarthritis of the Knee
NCT02057341PHASE2COMPLETEDA Study of ARRY-371797 in Patients With LMNA-Related Dilated Cardiomyopathy
NCT02351856PHASE2COMPLETEDA Rollover Study of ARRY-371797 in Patients With LMNA-Related Dilated Cardiomyopathy
NCT00729209PHASE1COMPLETEDA Study of ARRY-371797 in Patients With Rheumatoid Arthritis
NCT00790049PHASE1COMPLETEDA Safety Study of ARRY-371797 in Healthy Subjects

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

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.

65 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
AFATINIBChEMBL + PubChemPhase 4 (approved)MAPK14
REGORAFENIBChEMBL + PubChemPhase 4 (approved)MAPK14
3,3’,4’,5-TETRACHLOROSALICYLANILIDEChEMBLPhase 4 (approved)MAPK14
BENZBROMARONEChEMBLPhase 4 (approved)MAPK14
BITHIONOLChEMBLPhase 4 (approved)MAPK14
CELECOXIBChEMBLPhase 4 (approved)MAPK14
DASATINIBChEMBLPhase 4 (approved)MAPK14
DIETHYLSTILBESTROLChEMBLPhase 4 (approved)MAPK14
ENCORAFENIBChEMBLPhase 4 (approved)MAPK14
ETORICOXIBChEMBLPhase 4 (approved)MAPK14
GEFITINIBChEMBLPhase 4 (approved)MAPK14
HEXACHLOROPHENEChEMBLPhase 4 (approved)MAPK14
IMATINIBChEMBLPhase 4 (approved)MAPK14
ISOTRETINOINChEMBLPhase 4 (approved)MAPK14
LENVATINIBChEMBLPhase 4 (approved)MAPK14
MIFEPRISTONEChEMBLPhase 4 (approved)MAPK14
MONTELUKASTChEMBLPhase 4 (approved)MAPK14
NALFURAFINEChEMBLPhase 4 (approved)MAPK14
NELFINAVIRChEMBLPhase 4 (approved)MAPK14
NILOTINIBChEMBLPhase 4 (approved)MAPK14
PONATINIBChEMBLPhase 4 (approved)MAPK14
QUIZARTINIBChEMBLPhase 4 (approved)MAPK14
SORAFENIBChEMBLPhase 4 (approved)MAPK14
TANNIC ACIDChEMBLPhase 4 (approved)MAPK14
TOVORAFENIBChEMBLPhase 4 (approved)MAPK14
TRIBROMSALANChEMBLPhase 4 (approved)MAPK14
VANDETANIBChEMBLPhase 4 (approved)MAPK14
ZAFIRLUKASTChEMBLPhase 4 (approved)MAPK14
EPIGALOCATECHIN GALLATEChEMBLPhase 3MAPK14
LINIFANIBChEMBLPhase 3MAPK14
LOSMAPIMODChEMBLPhase 3MAPK14
PERIFOSINEChEMBLPhase 3MAPK14
TIRILAZADChEMBLPhase 3MAPK14
BAFETINIBChEMBLPhase 2MAPK14
BMS-582949ChEMBLPhase 2MAPK14
CEP-32496ChEMBLPhase 2MAPK14
CLOSANTELChEMBLPhase 2MAPK14
DIELDRINChEMBLPhase 2MAPK14
DORAMAPIMODChEMBLPhase 2MAPK14
FENBENDAZOLEChEMBLPhase 2MAPK14
FILAMINASTChEMBLPhase 2MAPK14
FORETINIBChEMBLPhase 2MAPK14
GALUNISERTIBChEMBLPhase 2MAPK14
GOLVATINIBChEMBLPhase 2MAPK14
ILORASERTIBChEMBLPhase 2MAPK14
IODOQUINOLChEMBLPhase 2MAPK14
ITX-5061 FREE BASEChEMBLPhase 2MAPK14
JNJ-49095397ChEMBLPhase 2MAPK14
MW-150ChEMBLPhase 2MAPK14
NAFENOPINChEMBLPhase 2MAPK14
NEFLAMAPIMODChEMBLPhase 2MAPK14
OSI-632ChEMBLPhase 2MAPK14
PAMAPIMODChEMBLPhase 2MAPK14
PEXMETINIBChEMBLPhase 2MAPK14
PH-797804ChEMBLPhase 2MAPK14
REBASTINIBChEMBLPhase 2MAPK14
TAK-715ChEMBLPhase 2MAPK14
TALMAPIMODChEMBLPhase 2MAPK14
TANZISERTIBChEMBLPhase 2MAPK14
TOP-1288ChEMBLPhase 2MAPK14