Camicinal
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Also known as GSK-962040GSK-962040BGsk962040GSK962040B
Summary
Camicinal (CHEMBL489095) is a phase-3 clinical-stage small molecule targeting MLNR; indicated across 1 condition including gastroparesis.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- Targets: 1 (MLNR)
- Indications: 1 condition
- Clinical trials: 7
- Chemistry: 424.6 Da · C25H33FN4O
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL489095 |
| Name | Camicinal |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 15984937 |
| Molecular formula | C25H33FN4O |
| Molecular weight | 424.6 |
| InChIKey | RZKDEGZIFSJVNA-IBGZPJMESA-N |
SMILES: C[C@H]1CN(CCN1)CC2=CC=C(C=C2)CC(=O)N3CCC(CC3)NC4=CC(=CC=C4)F
IUPAC name: 1-[4-(3-fluoroanilino)piperidin-1-yl]-2-[4-[[(3S)-3-methylpiperazin-1-yl]methyl]phenyl]ethanone
Also known as: Camicinal, GSK-962040, GSK-962040B, Gsk962040, GSK962040, GSK962040B, CAMICINAL
Parent form; salt/anhydrous children: CHEMBL489679
Patent coverage: 16 distinct patent families (44 SureChEMBL compound mentions), from 1 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
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 |
|---|---|---|---|---|---|
| MLNR | motilin receptor | Full agonist | 7.9 | 0.1% | O43193 |
Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Motilin receptor, Voltage-gated inwardly rectifying potassium channel KCNH2, Cytochrome P450 2D6, Cytochrome P450 3A4.
Bioactivity
ChEMBL activities: 2 potent at pChembl ≥ 5 of 6 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| MLNR | 7.9 | EC50 | 12.59 | nM | CHEMBL_ACT_2387383 |
| MLNR | 6.01 | EC50 | 970 | nM | CHEMBL_ACT_24839977 |
Target pathways
Aggregated over 1 target gene(s): MLNR.
Top Reactome pathways
7 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Signal Transduction | 1 | MLNR |
| Signaling by GPCR | 1 | MLNR |
| Class A/1 (Rhodopsin-like receptors) | 1 | MLNR |
| Peptide ligand-binding receptors | 1 | MLNR |
| GPCR downstream signalling | 1 | MLNR |
| G alpha (q) signalling events | 1 | MLNR |
| GPCR ligand binding | 1 | MLNR |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| G protein-coupled receptor signaling pathway | 1 |
| signal transduction | 1 |
Indications & clinical
Indications
1 indication (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).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| gastroparesis | 2 | MONDO:0006769 | EFO:1000948 |
Clinical trials
Total trials: 7.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 4 |
| PHASE1 | 3 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00861809 | PHASE2 | COMPLETED | The Effect of Single Doses of the Motilin Receptor Agonist GSK962040 in Type I Diabetic Patients With Gastroparesis |
| NCT01039805 | PHASE2 | COMPLETED | Evaluation of Single Doses of GSK962040 in Critically Ill Patients With Enteral Feed Intolerance |
| NCT01934192 | PHASE2 | TERMINATED | Nutritional Adequacy Therapeutic Enhancement in the Critically Ill. The NUTRIATE Study |
| NCT02210000 | PHASE2 | COMPLETED | A Study to Evaluate the Effect of Camicinal on Gastroparesis Symptoms in Type 1 and 2 Diabetic Subjects With Gastroparesis |
| NCT00562848 | PHASE1 | COMPLETED | A Study to Evaluate Safety, Side Effects, Muscle Activity and Speed of Gastric Emptying of GSK962040 |
| NCT00733551 | PHASE1 | COMPLETED | Evaluation of the Safety, Tolerability and Pharmacokinetics of Repeat Oral Doses of GSK962040 Administered to Healthy Adult Subjects. |
| NCT01039974 | PHASE1 | COMPLETED | GSK962040 Drug-drug Interaction Study With Ketoconazole |
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.
321 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| AMIODARONE | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| ATAZANAVIR | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| CANDESARTAN CILEXETIL | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| CARVEDILOL | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| CINACALCET | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| CLEMASTINE | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| CLOBETASOL PROPIONATE | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| CRIZOTINIB | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| ERYTHROMYCIN | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| FEDRATINIB | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| HYDROXYPROGESTERONE CAPROATE | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| PIMOZIDE | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| PONATINIB | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| SORAFENIB | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| TEGASEROD | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| TELOTRISTAT ETHYL | ChEMBL + PubChem | Phase 4 (approved) | MLNR |
| ACETOPHENAZINE | ChEMBL | Phase 4 (approved) | MLNR |
| AMPRENAVIR | ChEMBL | Phase 4 (approved) | MLNR |
| ARIPIPRAZOLE | ChEMBL | Phase 4 (approved) | MLNR |
| ASTEMIZOLE | ChEMBL | Phase 4 (approved) | MLNR |
| BAZEDOXIFENE | ChEMBL | Phase 4 (approved) | MLNR |
| BENPERIDOL | ChEMBL | Phase 4 (approved) | MLNR |
| BEPRIDIL | ChEMBL | Phase 4 (approved) | MLNR |
| CANNABIDIOL | ChEMBL | Phase 4 (approved) | MLNR |
| CHLORHEXIDINE | ChEMBL | Phase 4 (approved) | MLNR |
| CHLORPROTHIXENE | ChEMBL | Phase 4 (approved) | MLNR |
| CISAPRIDE | ChEMBL | Phase 4 (approved) | MLNR |
| DULOXETINE | ChEMBL | Phase 4 (approved) | MLNR |
| EBASTINE | ChEMBL | Phase 4 (approved) | MLNR |
| FENTICONAZOLE | ChEMBL | Phase 4 (approved) | MLNR |
| FLUSPIRILENE | ChEMBL | Phase 4 (approved) | MLNR |
| FLUTRIMAZOLE | ChEMBL | Phase 4 (approved) | MLNR |
| GLAFENINE | ChEMBL | Phase 4 (approved) | MLNR |
| INDOCYANINE GREEN ACID FORM | ChEMBL | Phase 4 (approved) | MLNR |
| ISRADIPINE | ChEMBL | Phase 4 (approved) | MLNR |
| LASOFOXIFENE | ChEMBL | Phase 4 (approved) | MLNR |
| NAFARELIN | ChEMBL | Phase 4 (approved) | MLNR |
| NEBIVOLOL | ChEMBL | Phase 4 (approved) | MLNR |
| NIMESULIDE | ChEMBL | Phase 4 (approved) | MLNR |
| NITAZOXANIDE | ChEMBL | Phase 4 (approved) | MLNR |
| NOSCAPINE | ChEMBL | Phase 4 (approved) | MLNR |
| OSIMERTINIB | ChEMBL | Phase 4 (approved) | MLNR |
| PERHEXILINE | ChEMBL | Phase 4 (approved) | MLNR |
| PROPIVERINE | ChEMBL | Phase 4 (approved) | MLNR |
| PYRVINIUM | ChEMBL | Phase 4 (approved) | MLNR |
| REBOXETINE | ChEMBL | Phase 4 (approved) | MLNR |
| RIFAXIMIN | ChEMBL | Phase 4 (approved) | MLNR |
| RIMONABANT | ChEMBL | Phase 4 (approved) | MLNR |
| RITONAVIR | ChEMBL | Phase 4 (approved) | MLNR |
| SERTINDOLE | ChEMBL | Phase 4 (approved) | MLNR |
| SERTRALINE | ChEMBL | Phase 4 (approved) | MLNR |
| SUNITINIB | ChEMBL | Phase 4 (approved) | MLNR |
| TACROLIMUS | ChEMBL | Phase 4 (approved) | MLNR |
| TIPRANAVIR | ChEMBL | Phase 4 (approved) | MLNR |
| TRIFLUOPERAZINE | ChEMBL | Phase 4 (approved) | MLNR |
| VILANTEROL | ChEMBL | Phase 4 (approved) | MLNR |
| VINDESINE | ChEMBL | Phase 4 (approved) | MLNR |
| AZELNIDIPINE | ChEMBL | Phase 3 | MLNR |
| BENIDIPINE | ChEMBL | Phase 3 | MLNR |
| CILNIDIPINE | ChEMBL | Phase 3 | MLNR |
Related Atlas pages
- Genes: MLNR
- Drugs: Amiodarone, Atazanavir, Candesartan Cilexetil, Carvedilol, Cinacalcet, Clemastine, Clobetasol Propionate, Crizotinib, Erythromycin, Fedratinib, Hydroxyprogesterone Caproate, Pimozide, Ponatinib, Sorafenib, Tegaserod, Telotristat Ethyl, Acetophenazine, Amprenavir, Aripiprazole, Astemizole, Bazedoxifene, Benperidol, Bepridil, Cannabidiol, Chlorhexidine, Chlorprothixene, Cisapride, Duloxetine, Ebastine, Fenticonazole, Fluspirilene, Flutrimazole, Glafenine, Indocyanine Green Acid Form, Isradipine, Lasofoxifene, Nafarelin, Nebivolol, Nimesulide, Nitazoxanide, Noscapine, Osimertinib, Perhexiline, Propiverine, Pyrvinium, Reboxetine, Rifaximin, Rimonabant, Ritonavir, Sertindole, Sertraline, Sunitinib, Tacrolimus, Tipranavir, Trifluoperazine, Vilanterol, Vindesine, Azelnidipine, Benidipine, Cilnidipine