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Reminertant

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Also known as MeclinertantSR-48692Sr48692SID124950704Merclinertant

Summary

Reminertant (CHEMBL506981) is a phase-3 clinical-stage small molecule targeting NTSR1 and NTSR2; indicated across 3 conditions including small cell lung carcinoma and lung neoplasm.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Targets: 2 (NTSR1, NTSR2)
  • Indications: 3 conditions
  • Clinical trials: 1
  • Chemistry: 587.1 Da · C32H31ClN4O5

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL506981
NameReminertant
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID119192
Molecular formulaC32H31ClN4O5
Molecular weight587.1
InChIKeyDYLJVOXRWLXDIG-UHFFFAOYSA-N

SMILES: COC1=C(C(=CC=C1)OC)C2=CC(=NN2C3=C4C=CC(=CC4=NC=C3)Cl)C(=O)NC5(C6CC7CC(C6)CC5C7)C(=O)O

IUPAC name: 2-[[1-(7-chloroquinolin-4-yl)-5-(2,6-dimethoxyphenyl)pyrazole-3-carbonyl]amino]adamantane-2-carboxylic acid

Also known as: Meclinertant, Reminertant, SR-48692, Sr48692, SID124950704, Merclinertant, REMINERTANT, MECLINERTANT, meclinertant

Patent coverage: 89 distinct patent families (235 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 194 (83%) 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
NTSR1NTS1 receptorAntagonist8.40%P30989
NTSR2NTS2 receptorFull agonist6.40.3%O95665

Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Neurotensin receptor type 2, Neurotensin receptor type 1, Sortilin, G-protein coupled receptor 183, Neurotensin receptor type 1, Neurotensin receptor type 2, N-formyl peptide receptor 3.

Bioactivity

ChEMBL activities: 17 potent at pChembl ≥ 5 of 18 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
NTSR19IC500.99nMCHEMBL_ACT_2275331
P207898.59Ki2.6nMCHEMBL_ACT_13374528
NTSR18.08Kd8.4nMCHEMBL_ACT_2487017
NTSR18.05Kd8.9nMCHEMBL_ACT_2487015
NTSR18.04Kd9.2nMCHEMBL_ACT_2487018
NTSR17.72Kd19nMCHEMBL_ACT_2487016
NTSR17.64Kd23nMCHEMBL_ACT_2487019
NTSR17.57Kd27nMCHEMBL_ACT_2487021
NTSR17.48Kd33nMCHEMBL_ACT_2487020
Q633847.21Ki62nMCHEMBL_ACT_14734772
NTSR17.09IC5082nMCHEMBL_ACT_15011316
P207897.09IC5082nMCHEMBL_ACT_19133768
Q633846.92EC50120nMCHEMBL_ACT_14734724
SORT16.62IC50238nMCHEMBL_ACT_13374526
NTSR26.38Ki418nMCHEMBL_ACT_13374527
FPR35.3IC504991nMCHEMBL_ACT_25751158
GPR1835.2IC506269nMCHEMBL_ACT_25751159

Target pathways

Aggregated over 2 target gene(s): NTSR1, NTSR2.

Top Reactome pathways

2 total, by targets touching each:

PathwayTargetsGenes
Peptide ligand-binding receptors2NTSR1, NTSR2
G alpha (q) signalling events2NTSR1, NTSR2

Dominant GO biological processes

GO termTargets
G protein-coupled receptor signaling pathway2
neuropeptide signaling pathway2
signal transduction2
temperature homeostasis1
negative regulation of systemic arterial blood pressure1
regulation of membrane depolarization1
cAMP biosynthetic process1
response to stress1
chemical synaptic transmission1
adult locomotory behavior1
positive regulation of gene expression1
positive regulation of glutamate secretion1
positive regulation of gamma-aminobutyric acid secretion1
response to food1
regulation of inositol trisphosphate biosynthetic process1

Indications & clinical

Indications

3 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
small cell lung carcinoma2MONDO:0008433EFO:0000702
lung neoplasm2MONDO:0021117MONDO:0008903

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

Clinical trials

Total trials: 1.

Phase distribution

PhaseTrials
PHASE2/PHASE31

Top trials by phase / activity

NCTPhaseStatusTitle
NCT00290953PHASE2/PHASE3COMPLETEDEvaluation of the Overall Survival of Meclinertant Versus Placebo After a First Line Chemotherapy With Cisplatin + Etoposide

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.

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

MoleculeSourceStatusShared targets
CAFFEINEChEMBL + PubChemPhase 4 (approved)NTSR1
DEXTROTHYROXINEChEMBLPhase 4 (approved)NTSR1
NILOTINIBChEMBLPhase 4 (approved)NTSR1
SORAFENIB TOSYLATEChEMBLPhase 4 (approved)NTSR1
TETRACAINEChEMBLPhase 4 (approved)NTSR1
THIMEROSALChEMBLPhase 3NTSR1
NORDAZEPAMChEMBLPhase 2NTSR1
AcetylcholinePubChemApprovedNTSR1
Aclidinium BromidePubChemApprovedNTSR1
AcyclovirPubChemApprovedNTSR1
Alendronic AcidPubChemApprovedNTSR1
AllopurinolPubChemApprovedNTSR1
AlogliptinPubChemApprovedNTSR1
AlprazolamPubChemApprovedNTSR1
AmiloridePubChemApprovedNTSR1
AmitriptylinePubChemApprovedNTSR1
AmlodipinePubChemApprovedNTSR1
AmoxapinePubChemApprovedNTSR1
AmoxicillinPubChemApprovedNTSR1
AmphetaminePubChemApprovedNTSR1
AspirinPubChemApprovedNTSR1
AzathioprinePubChemApprovedNTSR1
azithromycin, unspecified formPubChemApprovedNTSR1
BaclofenPubChemApprovedNTSR1
BeclomethasonePubChemApprovedNTSR1
Beclomethasone DipropionatePubChemApprovedNTSR1
BelzutifanPubChemApprovedNTSR1
BicalutamidePubChemApprovedNTSR1
BisoprololPubChemApprovedNTSR1
BosentanPubChemApprovedNTSR1
BromocriptinePubChemApprovedNTSR1
BumetanidePubChemApprovedNTSR1
BupropionPubChemApprovedNTSR1
CandesartanPubChemApprovedNTSR1
Candesartan CilexetilPubChemApprovedNTSR1
CarisoprodolPubChemApprovedNTSR1
CarvedilolPubChemApprovedNTSR1
CelecoxibPubChemApprovedNTSR1
cephalexinPubChemApprovedNTSR1
CetirizinePubChemApprovedNTSR1
chlorpheniraminePubChemApprovedNTSR1
ChlorpromazinePubChemApprovedNTSR1
CimetidinePubChemApprovedNTSR1
CiprofloxacinPubChemApprovedNTSR1
CitalopramPubChemApprovedNTSR1
ClindamycinPubChemApprovedNTSR1
ClonazepamPubChemApprovedNTSR1
ClonidinePubChemApprovedNTSR1
ClotrimazolePubChemApprovedNTSR1
ClozapinePubChemApprovedNTSR1
CyclobenzaprinePubChemApprovedNTSR1
DesloratadinePubChemApprovedNTSR1
dexamethasonePubChemApprovedNTSR1
DiazepamPubChemApprovedNTSR1
DiclofenacPubChemApprovedNTSR1
DiethylstilbestrolPubChemApprovedNTSR1
DihydroergotaminePubChemApprovedNTSR1
DiltiazemPubChemApprovedNTSR1
DiphenhydraminePubChemApprovedNTSR1
DipyridamolePubChemApprovedNTSR1

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot