Remission & chronicity
Biomarker Targets & Therapeutic Agents
Gene targets queried against DGIdb, Open Targets, ChEMBL, PubMed, and Europe PMC. Agents ranked: Clinical > Mechanistic > Correlative.
ADORA2A
| Therapeutic Agent | Effect Direction | Evidence Tier | Potency | Source |
|---|---|---|---|---|
| CIFORADENANT | ↓ inhibits | Mechanistic | DGIdb | |
| PSB36 | ↓ inhibits | Mechanistic | DGIdb | |
| THEOPHYLLINE | ↓ inhibits | Mechanistic | 28200.0 nM (EC50) | DGIdb |
| REGADENOSON ANHYDROUS | ↑ activates | Mechanistic | DGIdb | |
| [3H]CGS 21680 | ↑ activates | Mechanistic | DGIdb | |
| CV-1808 | ↑ activates | Mechanistic | DGIdb | |
| MRS5151 | ↑ activates | Mechanistic | DGIdb | |
| TOZADENANT | ↓ inhibits | Mechanistic | DGIdb | |
| PBF-509 | ↓ inhibits | Mechanistic | DGIdb | |
| CAFFEINE | ↓ inhibits | Mechanistic | DGIdb | |
| ISTRADEFYLLINE | ↓ inhibits | Mechanistic | DGIdb | |
| MRS1093 | ↓ inhibits | Mechanistic | DGIdb | |
| SONEDENOSON | ↑ activates | Mechanistic | DGIdb | |
| APADENOSON | ↑ activates | Mechanistic | DGIdb | |
| MRS1086 | ↓ inhibits | Mechanistic | DGIdb | |
| ST-1535 | ↓ inhibits | Mechanistic | DGIdb | |
| (S)-PIA | ↑ activates | Mechanistic | DGIdb | |
| MRE 3008F20 | ↓ inhibits | Mechanistic | DGIdb | |
| BINODENOSON | ↑ activates | Mechanistic | DGIdb | |
| PENTOXIFYLLINE | ↓ inhibits | Mechanistic | DGIdb | |
| LUF7602 | ↓ inhibits | Mechanistic | DGIdb | |
| ETRUMADENANT | ↓ inhibits | Mechanistic | DGIdb | |
| MRS1088 | ↓ inhibits | Mechanistic | DGIdb | |
| OXTRIPHYLLINE | ↓ inhibits | Mechanistic | DGIdb | |
| ATL802 | ↓ inhibits | Mechanistic | DGIdb | |
| DEXEFAROXAN | ? unclear | Mechanistic | DGIdb | |
| CAFFEINE CITRATE | ↓ inhibits | Mechanistic | DGIdb | |
| UK-432,097 | ↑ activates | Mechanistic | DGIdb | |
| KF26777 | ↓ inhibits | Mechanistic | DGIdb | |
| MRS1041 | ↓ inhibits | Mechanistic | DGIdb | |
| LEVODOPA | ? unclear | Mechanistic | DGIdb | |
| XANTHINE AMINE CONGENER | ↓ inhibits | Mechanistic | 18.4 nM (Ki) | DGIdb |
| DEFIBROTIDE | ↑ activates | Mechanistic | DGIdb | |
| EVODENOSON | ↑ activates | Mechanistic | DGIdb | |
| IMARADENANT | ↓ inhibits | Mechanistic | DGIdb | |
| GALANGIN | ↓ inhibits | Mechanistic | DGIdb | |
| LAS38096 | ↓ inhibits | Mechanistic | DGIdb | |
| GS9667 | ↑ activates | Mechanistic | DGIdb | |
| N(6)-CYCLOHEXYLADENOSINE | ↑ activates | Mechanistic | DGIdb | |
| BVT.115959 | ↑ activates | Mechanistic | DGIdb |
Showing top 40 of 283 agents ranked by evidence tier.
GABRA1
| Therapeutic Agent | Effect Direction | Evidence Tier | Potency | Source |
|---|---|---|---|---|
| PICROTOXIN | ? unclear | Mechanistic | DGIdb | |
| THIAMYLAL SODIUM | ~ modulates | Mechanistic | DGIdb | |
| GANAXOLONE | ~ modulates | Mechanistic | DGIdb | |
| BUTOBARBITAL | ? unclear | Mechanistic | DGIdb | |
| CHLORDIAZEPOXIDE | ~ modulates | Mechanistic | DGIdb | |
| CLOBAZAM | ~ modulates | Mechanistic | DGIdb | |
| CLORAZEPATE | ? unclear | Mechanistic | DGIdb | |
| TPA023 | ~ modulates | Mechanistic | DGIdb | |
| ZK-93423 | ? unclear | Mechanistic | DGIdb | |
| FLUMAZENIL | ~ modulates | Mechanistic | 3.3 nM (Ki) | DGIdb |
| AMOBARBITAL | ? unclear | Mechanistic | DGIdb | |
| PAGOCLONE | ~ modulates | Mechanistic | DGIdb | |
| OXAZEPAM | ~ modulates | Mechanistic | DGIdb | |
| TETRAHYDRODEOXYCORTICOSTERONE | ~ modulates | Mechanistic | DGIdb | |
| METHOHEXITAL | ? unclear | Mechanistic | DGIdb | |
| CLONAZEPAM | ~ modulates | Mechanistic | DGIdb | |
| [3H]GABAZINE | ↓ inhibits | Mechanistic | DGIdb | |
| FLURAZEPAM | ? unclear | Mechanistic | DGIdb | |
| METHARBITAL | ~ modulates | Mechanistic | DGIdb | |
| LORAZEPAM | ~ modulates | Mechanistic | DGIdb | |
| RO4938581 | ~ modulates | Mechanistic | DGIdb | |
| SECOBARBITAL | ? unclear | Mechanistic | DGIdb | |
| BUTABARBITAL SODIUM | ~ modulates | Mechanistic | DGIdb | |
| MIDAZOLAM HYDROCHLORIDE | ~ modulates | Mechanistic | DGIdb | |
| SANDARACOPIMARIC ACID | ? unclear | Mechanistic | DGIdb | |
| QUAZEPAM | ~ modulates | Mechanistic | DGIdb | |
| PHENOBARBITAL | ? unclear | Mechanistic | DGIdb | |
| PRIMIDONE | ~ modulates | Mechanistic | DGIdb | |
| ISOGUVACINE | ↑ activates | Mechanistic | DGIdb | |
| ZOLPIDEM TARTRATE | ~ modulates | Mechanistic | DGIdb | |
| CHEMBL:CHEMBL2170369 | ? unclear | Mechanistic | DGIdb | |
| ESTAZOLAM | ~ modulates | Mechanistic | DGIdb | |
| TOPIRAMATE | ~ modulates | Mechanistic | DGIdb | |
| ETHCHLORVYNOL | ~ modulates | Mechanistic | DGIdb | |
| CLORAZEPATE DIPOTASSIUM | ~ modulates | Mechanistic | DGIdb | |
| ZALEPLON | ~ modulates | Mechanistic | DGIdb | |
| FLUNITRAZEPAM | ~ modulates | Mechanistic | 4.5 nM (Kd) | DGIdb |
| BUTABARBITAL | ? unclear | Mechanistic | DGIdb | |
| THIAMYLAL | ? unclear | Mechanistic | DGIdb | |
| BUTALBITAL | ~ modulates | Mechanistic | DGIdb |
Showing top 40 of 302 agents ranked by evidence tier.
GABRA2
| Therapeutic Agent | Effect Direction | Evidence Tier | Potency | Source |
|---|---|---|---|---|
| OCINAPLON | ~ modulates | Mechanistic | DGIdb | |
| FLUNITRAZEPAM | ~ modulates | Mechanistic | DGIdb | |
| PAGOCLONE | ? unclear | Mechanistic | DGIdb | |
| LORAZEPAM | ~ modulates | Mechanistic | DGIdb | |
| PRIMIDONE | ~ modulates | Mechanistic | DGIdb | |
| PICROTOXIN | ↓ inhibits | Mechanistic | DGIdb | |
| BROMAZEPAM | ~ modulates | Mechanistic | DGIdb | |
| DEXMEDETOMIDINE HYDROCHLORIDE | ? unclear | Mechanistic | DGIdb | |
| TOPIRAMATE | ~ modulates | Mechanistic | DGIdb | |
| ZOLPIDEM TARTRATE | ~ modulates | Mechanistic | DGIdb | |
| ZOPICLONE | ~ modulates | Mechanistic | DGIdb | |
| ESZOPICLONE | ~ modulates | Mechanistic | DGIdb | |
| AZD7325 | ~ modulates | Mechanistic | 0.3 nM (Ki) | DGIdb |
| Α5IA | ~ modulates | Mechanistic | DGIdb | |
| PRAZEPAM | ~ modulates | Mechanistic | DGIdb | |
| METHOHEXITAL SODIUM | ~ modulates | Mechanistic | DGIdb | |
| ACAMPROSATE CALCIUM | ~ modulates | Mechanistic | DGIdb | |
| DIAZEPAM | ~ modulates | Mechanistic | 17.0 nM (Ki) | DGIdb |
| RO4938581 | ~ modulates | Mechanistic | DGIdb | |
| PENTOBARBITAL SODIUM | ~ modulates | Mechanistic | DGIdb | |
| MEPROBAMATE | ↑ activates | Mechanistic | DGIdb | |
| FLUMAZENIL | ~ modulates | Mechanistic | 0.7943 nM (Ki) | DGIdb |
| [18F]FLUOROETHYLFLUMAZENIL | ~ modulates | Mechanistic | DGIdb | |
| CLOMETHIAZOLE | ~ modulates | Mechanistic | DGIdb | |
| GANAXOLONE | ~ modulates | Mechanistic | DGIdb | |
| BRETAZENIL | ~ modulates | Mechanistic | DGIdb | |
| THIOPENTAL | ? unclear | Mechanistic | DGIdb | |
| HEXOBARBITAL | ? unclear | Mechanistic | DGIdb | |
| OXAZEPAM | ~ modulates | Mechanistic | DGIdb | |
| FLURAZEPAM | ? unclear | Mechanistic | DGIdb | |
| IMEPITOIN | ↑ activates | Mechanistic | DGIdb | |
| TRIAZOLAM | ~ modulates | Mechanistic | DGIdb | |
| BUTALBITAL | ~ modulates | Mechanistic | DGIdb | |
| ALPRAZOLAM | ~ modulates | Mechanistic | 12.0 nM (EC50) | DGIdb |
| HALOTHANE | ~ modulates | Mechanistic | DGIdb | |
| ADIPIPLON | ↑ activates | Mechanistic | DGIdb | |
| ISOFLURANE | ~ modulates | Mechanistic | DGIdb | |
| TALBUTAL | ~ modulates | Mechanistic | DGIdb | |
| CIPEPOFOL | ↑ activates | Mechanistic | DGIdb | |
| CLORAZEPATE DIPOTASSIUM | ~ modulates | Mechanistic | DGIdb |
Showing top 40 of 264 agents ranked by evidence tier.
HCRTR1
| Therapeutic Agent | Effect Direction | Evidence Tier | Potency | Source |
|---|---|---|---|---|
| FILOREXANT | ↓ inhibits | Mechanistic | DGIdb | |
| SUVOREXANT | ↓ inhibits | Mechanistic | DGIdb | |
| FIRAZOREXTON | ↑ activates | Mechanistic | DGIdb | |
| RTOXA-43 | ↑ activates | Mechanistic | DGIdb | |
| JH112 | ↓ inhibits | Mechanistic | DGIdb | |
| [3H]-ALMOREXANT | ↓ inhibits | Mechanistic | DGIdb | |
| [3H]SB-674042 | ↓ inhibits | Mechanistic | DGIdb | |
| OREXIN-B | ↑ activates | Mechanistic | DGIdb | |
| CHEMBL:CHEMBL1520346 | ? unclear | Mechanistic | DGIdb | |
| [125I]OREXIN A (HUMAN, MOUSE, RAT) | ? unclear | Mechanistic | DGIdb | |
| OVEPOREXTON | ↑ activates | Mechanistic | DGIdb | |
| ORN-0829 HYDRATE | ↓ inhibits | Mechanistic | DGIdb | |
| TCS 1102 | ↓ inhibits | Mechanistic | DGIdb | |
| [ALA11, D-LEU15]OREXIN-B | ↑ activates | Mechanistic | DGIdb | |
| YNT-185 | ↑ activates | Mechanistic | DGIdb | |
| SB-334867 | ↓ inhibits | Mechanistic | DGIdb | |
| EMPA | ↓ inhibits | Mechanistic | DGIdb | |
| COMPOUND 11 [PMID: 15261275] | ↓ inhibits | Mechanistic | DGIdb | |
| OREXIN-A | ↑ activates | Mechanistic | DGIdb | |
| ACT-335827 | ↓ inhibits | Mechanistic | DGIdb | |
| SB-408124 | ↓ inhibits | Mechanistic | DGIdb | |
| MK-1064 | ↓ inhibits | Mechanistic | DGIdb | |
| SB-649868 | ? unclear | Mechanistic | DGIdb | |
| MK-3697 | ↓ inhibits | Mechanistic | DGIdb | |
| FAZAMOREXANT | ↓ inhibits | Mechanistic | DGIdb | |
| LEMBOREXANT | ↓ inhibits | Mechanistic | DGIdb | |
| LSN2424100 | ↓ inhibits | Mechanistic | DGIdb | |
| SB-410220 | ↓ inhibits | Mechanistic | DGIdb | |
| SELTOREXANT | ↓ inhibits | Mechanistic | DGIdb | |
| DARIDOREXANT HYDROCHLORIDE | ↓ inhibits | Mechanistic | DGIdb | |
| DANAVOREXTON | ↑ activates | Mechanistic | DGIdb | |
| [3H]-TCS 1102 | ↓ inhibits | Mechanistic | DGIdb | |
| HTL6641 | ↓ inhibits | Mechanistic | DGIdb | |
| 1-SORA-51 | ↓ inhibits | Mechanistic | DGIdb | |
| DARIDOREXANT | ↓ inhibits | Mechanistic | DGIdb | |
| NIVASOREXANT | ? unclear | Mechanistic | DGIdb | |
| ALMOREXANT | ↓ inhibits | Mechanistic | 13.0 nM (IC50) | DGIdb |
| SB-674042 | ↓ inhibits | Mechanistic | DGIdb | |
| CVN45502 | ↓ inhibits | Mechanistic | DGIdb | |
| COMPOUND 1 [PMID: 33547286] | ↑ activates | Mechanistic | DGIdb |
Showing top 40 of 233 agents ranked by evidence tier.
HCRTR2
| Therapeutic Agent | Effect Direction | Evidence Tier | Potency | Source |
|---|---|---|---|---|
| DARIDOREXANT | ↓ inhibits | Mechanistic | DGIdb | |
| TCS 1102 | ↓ inhibits | Mechanistic | DGIdb | |
| FILOREXANT | ↓ inhibits | Mechanistic | DGIdb | |
| T-516 | ↑ activates | Mechanistic | DGIdb | |
| OREXIN-A | ↑ activates | Mechanistic | DGIdb | |
| ACT-335827 | ↓ inhibits | Mechanistic | DGIdb | |
| MK-3697 | ↓ inhibits | Mechanistic | DGIdb | |
| ACT-462206 | ↓ inhibits | Mechanistic | DGIdb | |
| EMPA | ↓ inhibits | Mechanistic | DGIdb | |
| OVEPOREXTON | ↑ activates | Mechanistic | DGIdb | |
| RTOXA-43 | ↑ activates | Mechanistic | DGIdb | |
| FIRAZOREXTON | ↑ activates | Mechanistic | DGIdb | |
| HTL6641 | ↓ inhibits | Mechanistic | DGIdb | |
| DANAVOREXTON | ↑ activates | Mechanistic | DGIdb | |
| SELTOREXANT | ↓ inhibits | Mechanistic | DGIdb | |
| COMPOUND 1 [PMID: 33547286] | ↑ activates | Mechanistic | DGIdb | |
| [3H]-TCS 1102 | ↓ inhibits | Mechanistic | DGIdb | |
| FAZAMOREXANT | ↓ inhibits | Mechanistic | DGIdb | |
| ORN-0829 HYDRATE | ↓ inhibits | Mechanistic | DGIdb | |
| CP-1 | ↓ inhibits | Mechanistic | DGIdb | |
| [3H]EMPA | ↓ inhibits | Mechanistic | DGIdb | |
| SB-649868 | ↓ inhibits | Mechanistic | DGIdb | |
| (R)-YNT-3708 | ↑ activates | Mechanistic | DGIdb | |
| VORNOREXANT | ↓ inhibits | Mechanistic | DGIdb | |
| SUVOREXANT | ↓ inhibits | Mechanistic | DGIdb | |
| SB-674042 | ↓ inhibits | Mechanistic | DGIdb | |
| ALIXOREXTON | ↑ activates | Mechanistic | DGIdb | |
| [3H]-ALMOREXANT | ↓ inhibits | Mechanistic | DGIdb | |
| SB-334867 | ↓ inhibits | Mechanistic | DGIdb | |
| [125I]OREXIN A (HUMAN, MOUSE, RAT) | ? unclear | Mechanistic | DGIdb | |
| YNT-185 | ↑ activates | Mechanistic | DGIdb | |
| TCS-OX2-29 | ↓ inhibits | Mechanistic | DGIdb | |
| CVN45502 | ↓ inhibits | Mechanistic | DGIdb | |
| [3H]T-516 | ↑ activates | Mechanistic | DGIdb | |
| LEMBOREXANT | ↓ inhibits | Mechanistic | DGIdb | |
| [3H]SB-674042 | ↓ inhibits | Mechanistic | DGIdb | |
| LSN2424100 | ↓ inhibits | Mechanistic | DGIdb | |
| ALMOREXANT | ↓ inhibits | Mechanistic | DGIdb | |
| NAG 26 | ↑ activates | Mechanistic | DGIdb | |
| [ALA11, D-LEU15]OREXIN-B | ↑ activates | Mechanistic | DGIdb |
Showing top 40 of 245 agents ranked by evidence tier.
HRH1
| Therapeutic Agent | Effect Direction | Evidence Tier | Potency | Source |
|---|---|---|---|---|
| HISTAMINE | ↑ activates | Mechanistic | 13.0 nM (EC50) | DGIdb |
| RISPERIDONE | ↓ inhibits | Mechanistic | 2.6 nM (Ki) | DGIdb |
| EPINASTINE | ↓ inhibits | Mechanistic | DGIdb | |
| PYRILAMINE | ↓ inhibits | Mechanistic | 12.59 nM (IC50) | DGIdb |
| ORPHENADRINE | ? unclear | Mechanistic | DGIdb | |
| MIZOLASTINE | ↓ inhibits | Mechanistic | DGIdb | |
| BETAHISTINE | ↑ activates | Mechanistic | DGIdb | |
| METHAPYRILENE FUMARATE | ↓ inhibits | Mechanistic | DGIdb | |
| MIANSERIN | ? unclear | Mechanistic | 3.388 nM (IC50) | DGIdb |
| MEQUITAZINE | ↓ inhibits | Mechanistic | DGIdb | |
| SERTINDOLE | ↓ inhibits | Mechanistic | 570.0 nM (Ki) | DGIdb |
| BROMPHENIRAMINE | ? unclear | Mechanistic | DGIdb | |
| LORATADINE | ↓ inhibits | Mechanistic | DGIdb | |
| TRIMEPRAZINE | ? unclear | Mechanistic | DGIdb | |
| BU-E 47 | ↓ inhibits | Mechanistic | DGIdb | |
| DEXCHLORPHENIRAMINE MALEATE | ? unclear | Mechanistic | DGIdb | |
| AZELASTINE | ↓ inhibits | Mechanistic | DGIdb | |
| ASENAPINE | ↓ inhibits | Mechanistic | DGIdb | |
| BROMODIPHENHYDRAMINE | ? unclear | Mechanistic | DGIdb | |
| OLOPATADINE HYDROCHLORIDE | ↓ inhibits | Mechanistic | DGIdb | |
| BEPOTASTINE BESILATE | ? unclear | Mechanistic | DGIdb | |
| FEXOFENADINE HYDROCHLORIDE | ↓ inhibits | Mechanistic | DGIdb | |
| PROPIOMAZINE | ? unclear | Mechanistic | DGIdb | |
| CETIRIZINE HYDROCHLORIDE | ↓ inhibits | Mechanistic | DGIdb | |
| DIPHENHYDRAMINE | ↓ inhibits | Mechanistic | DGIdb | |
| ARPROMIDINE | ↓ inhibits | Mechanistic | DGIdb | |
| PHENIRAMINE | ? unclear | Mechanistic | DGIdb | |
| QUETIAPINE FUMARATE | ↓ inhibits | Mechanistic | DGIdb | |
| AZATADINE | ? unclear | Mechanistic | DGIdb | |
| DOXEPIN HYDROCHLORIDE | ↓ inhibits | Mechanistic | DGIdb | |
| TRIPROLIDINE | ↓ inhibits | Mechanistic | DGIdb | |
| PROMETHAZINE HYDROCHLORIDE | ↓ inhibits | Mechanistic | DGIdb | |
| HYDROXYZINE | ↓ inhibits | Mechanistic | DGIdb | |
| ILOPERIDONE | ? unclear | Mechanistic | DGIdb | |
| PEMIROLAST | ? unclear | Mechanistic | DGIdb | |
| CHLORPHENIRAMINE POLISTIREX | ↓ inhibits | Mechanistic | DGIdb | |
| DIMETHINDENE | ↓ inhibits | Mechanistic | 0.6918 nM (Ki) | DGIdb |
| VAPITADINE | ? unclear | Mechanistic | DGIdb | |
| ARIPIPRAZOLE LAUROXIL | ↓ inhibits | Mechanistic | DGIdb | |
| BRILAROXAZINE | ? unclear | Mechanistic | DGIdb |
Showing top 40 of 374 agents ranked by evidence tier.
HTR2A
| Therapeutic Agent | Effect Direction | Evidence Tier | Potency | Source |
|---|---|---|---|---|
| LURASIDONE HYDROCHLORIDE | ? unclear | Mechanistic | DGIdb | |
| ESMIRTAZAPINE | ? unclear | Mechanistic | DGIdb | |
| PERGOLIDE | ↑ activates | Mechanistic | DGIdb | |
| XANOMELINE | ↓ inhibits | Mechanistic | DGIdb | |
| BROLAMFETAMINE | ↑ activates | Mechanistic | 41.0 nM (Ki) | DGIdb |
| BRL-15572 | ↑ activates | Mechanistic | DGIdb | |
| ARIPIPRAZOLE LAUROXIL | ↓ inhibits | Mechanistic | DGIdb | |
| MIANSERIN | ↓ inhibits | Mechanistic | DGIdb | |
| [3H]8-OH-DPAT | ↑ activates | Mechanistic | DGIdb | |
| OLANZAPINE | ↓ inhibits | Mechanistic | DGIdb | |
| SB 228357 | ↓ inhibits | Mechanistic | DGIdb | |
| 5-HYDROXYTRYPTAMINE | ↑ activates | Mechanistic | DGIdb | |
| HALOPERIDOL LACTATE | ↓ inhibits | Mechanistic | DGIdb | |
| METHYLERGONOVINE | ↑ activates | Mechanistic | DGIdb | |
| QUIPAZINE | ↑ activates | Mechanistic | DGIdb | |
| ASENAPINE | ↓ inhibits | Mechanistic | DGIdb | |
| FLUPHENAZINE HYDROCHLORIDE | ↓ inhibits | Mechanistic | DGIdb | |
| LUMATEPERONE | ↓ inhibits | Mechanistic | DGIdb | |
| TRIFLUOPERAZINE | ↓ inhibits | Mechanistic | DGIdb | |
| KETANSERIN | ↓ inhibits | Mechanistic | DGIdb | |
| LOXAPINE | ↓ inhibits | Mechanistic | DGIdb | |
| VER-3323 | ↑ activates | Mechanistic | DGIdb | |
| SARPOGRELATE | ↓ inhibits | Mechanistic | DGIdb | |
| BREXPIPRAZOLE | ↓ inhibits | Mechanistic | DGIdb | |
| EPLIVANSERIN | ? unclear | Mechanistic | DGIdb | |
| PROMAZINE HYDROCHLORIDE | ↓ inhibits | Mechanistic | DGIdb | |
| TRAZODONE | ↓ inhibits | Mechanistic | DGIdb | |
| MOLINDONE HYDROCHLORIDE | ↓ inhibits | Mechanistic | DGIdb | |
| BLONANSERIN | ↓ inhibits | Mechanistic | DGIdb | |
| MOLINDONE | ↓ inhibits | Mechanistic | DGIdb | |
| 9-OH-RISPERIDONE | ↓ inhibits | Mechanistic | DGIdb | |
| PRUVANSERIN | ↓ inhibits | Mechanistic | DGIdb | |
| QUETIAPINE FUMARATE | ↓ inhibits | Mechanistic | DGIdb | |
| NEFAZODONE | ↓ inhibits | Mechanistic | DGIdb | |
| BW723C86 | ↑ activates | Mechanistic | DGIdb | |
| MESORIDAZINE | ↓ inhibits | Mechanistic | DGIdb | |
| ORG 12962 | ↑ activates | Mechanistic | DGIdb | |
| FLIBANSERIN | ↓ inhibits | Mechanistic | DGIdb | |
| LP-12 | ↑ activates | Mechanistic | DGIdb | |
| MESORIDAZINE BESYLATE | ↓ inhibits | Mechanistic | DGIdb |
Showing top 40 of 362 agents ranked by evidence tier.
MTNR1A
| Therapeutic Agent | Effect Direction | Evidence Tier | Potency | Source |
|---|---|---|---|---|
| AZD7325 | ↓ inhibits | Mechanistic | DGIdb | |
| UCM 549 | ↓ inhibits | Mechanistic | DGIdb | |
| S20928 | ↓ inhibits | Mechanistic | DGIdb | |
| IIK7 | ↑ activates | Mechanistic | DGIdb | |
| MELATONIN | ↑ activates | Mechanistic | 0.4 nM (Ki) | DGIdb |
| S26284 | ↑ activates | Mechanistic | DGIdb | |
| S24773 | ↑ activates | Mechanistic | DGIdb | |
| AGOMELATINE | ↑ activates | Mechanistic | 0.06 nM (Ki) | DGIdb |
| 2-METHOXY-Α,Β-DIDEHYDRO-AGOMELATINE | ↑ activates | Mechanistic | DGIdb | |
| RAMELTEON | ↑ activates | Mechanistic | 0.0138 nM (Ki) | DGIdb |
| UCSF4226 | ↑ activates | Mechanistic | DGIdb | |
| TASIMELTEON | ↑ activates | Mechanistic | DGIdb | |
| GR 196429 | ↑ activates | Mechanistic | DGIdb | |
| UCM 793 | ↑ activates | Mechanistic | DGIdb | |
| PIROMELATINE | ↑ activates | Mechanistic | DGIdb | |
| S24014 | ↑ activates | Mechanistic | DGIdb | |
| S22153 | ↓ inhibits | Mechanistic | DGIdb | |
| EFPPEA | ↑ activates | Mechanistic | DGIdb | |
| UCSF3384 | ↑ activates | Mechanistic | DGIdb | |
| LUZINDOLE | ↓ inhibits | Mechanistic | DGIdb | |
| [125I]SD6 | ↑ activates | Mechanistic | DGIdb | |
| 2-[125I]MELATONIN | ↑ activates | Mechanistic | DGIdb | |
| 4P-PDOT | ↓ inhibits | Mechanistic | DGIdb | |
| 5-HEAT | ↑ activates | Mechanistic | DGIdb | |
| UCM 724 | ↓ inhibits | Mechanistic | DGIdb | |
| 6-CL-MLT | ↑ activates | Mechanistic | DGIdb | |
| N-[2-(2-IODO-5-METHOXY-1H-INDOL-3-YL)ETHYL]ACETAMIDE | ↑ activates | Mechanistic | DGIdb | |
| UCM1341 | ↑ activates | Mechanistic | DGIdb | |
| S26131 | ↓ inhibits | Mechanistic | DGIdb | |
| AAE-M-PBP-AMINE | ↑ activates | Mechanistic | DGIdb | |
| 6-HYDROXYMELATONIN | ↑ activates | Mechanistic | DGIdb | |
| GR 128107 | ↑ activates | Mechanistic | DGIdb | |
| K185 | ↓ inhibits | Mechanistic | DGIdb | |
| ICOA-13 | ↑ activates | Mechanistic | DGIdb | |
| TIK-301 | ? unclear | Mechanistic | DGIdb | |
| DIFLUOROAGOMELATINE | ↑ activates | Mechanistic | DGIdb | |
| LY 156735 | ↑ activates | Mechanistic | DGIdb | |
| UCSF7447 | ↓ inhibits | Mechanistic | DGIdb | |
| CBOBNEA | ↑ activates | Mechanistic | DGIdb | |
| CHEMBL127565 | ↓ inhibits | Mechanistic | 492.0 nM (Ki) | ChEMBL |
Showing top 40 of 207 agents ranked by evidence tier.
MTNR1B
| Therapeutic Agent | Effect Direction | Evidence Tier | Potency | Source |
|---|---|---|---|---|
| LUZINDOLE | ↓ inhibits | Mechanistic | DGIdb | |
| S20928 | ↓ inhibits | Mechanistic | DGIdb | |
| UCSF3384 | ↑ activates | Mechanistic | DGIdb | |
| ISOAMYL-AGOMELATINE | ↑ activates | Mechanistic | DGIdb | |
| TASIMELTEON | ↑ activates | Mechanistic | DGIdb | |
| AGOMELATINE | ↑ activates | Mechanistic | 0.27 nM (Ki) | DGIdb |
| S22153 | ↑ activates | Mechanistic | DGIdb | |
| IIK7 | ↑ activates | Mechanistic | DGIdb | |
| [125I]SD6 | ↑ activates | Mechanistic | DGIdb | |
| BOMPPA | ↑ activates | Mechanistic | DGIdb | |
| 4P-PDOT | ↓ inhibits | Mechanistic | DGIdb | |
| UCM 549 | ↓ inhibits | Mechanistic | DGIdb | |
| (HYDROXYMETHYLPHENYL)AGOMELATINE | ↓ inhibits | Mechanistic | DGIdb | |
| UCSF7447 | ↑ activates | Mechanistic | DGIdb | |
| GR 196429 | ↑ activates | Mechanistic | DGIdb | |
| S26284 | ↑ activates | Mechanistic | DGIdb | |
| S26131 | ↓ inhibits | Mechanistic | DGIdb | |
| ICOA-13 | ↑ activates | Mechanistic | DGIdb | |
| MELATONIN | ↑ activates | Mechanistic | 0.3 nM (Ki) | DGIdb |
| 5-HEAT | ↓ inhibits | Mechanistic | DGIdb | |
| UCM1341 | ↑ activates | Mechanistic | DGIdb | |
| S24014 | ↑ activates | Mechanistic | DGIdb | |
| PIROMELATINE | ↑ activates | Mechanistic | DGIdb | |
| 2-[125I]MELATONIN | ↑ activates | Mechanistic | DGIdb | |
| UCM 765 | ↑ activates | Mechanistic | DGIdb | |
| S24773 | ↑ activates | Mechanistic | DGIdb | |
| GR 128107 | ↑ activates | Mechanistic | DGIdb | |
| CIFEA | ↑ activates | Mechanistic | DGIdb | |
| VINCRISTINE | ? unclear | Mechanistic | DGIdb | |
| 2-(INDOLIN-1YL)-MELATONIN | ↓ inhibits | Mechanistic | DGIdb | |
| LY 156735 | ↑ activates | Mechanistic | DGIdb | |
| N-[2-(2-IODO-5-METHOXY-1H-INDOL-3-YL)ETHYL]ACETAMIDE | ↑ activates | Mechanistic | DGIdb | |
| UCM1014 | ↑ activates | Mechanistic | DGIdb | |
| 6-HYDROXYMELATONIN | ↑ activates | Mechanistic | DGIdb | |
| [125I]S70254 | ↑ activates | Mechanistic | DGIdb | |
| RAMELTEON | ↑ activates | Mechanistic | 0.045 nM (Ki) | DGIdb |
| UCM 724 | ↓ inhibits | Mechanistic | DGIdb | |
| UCSF4226 | ↑ activates | Mechanistic | DGIdb | |
| 6-CL-MLT | ↑ activates | Mechanistic | DGIdb | |
| DH97 | ↓ inhibits | Mechanistic | DGIdb |
Showing top 40 of 220 agents ranked by evidence tier.
Clinical Trials
Drug, biologic and supplement trials (treatment or prevention) from ClinicalTrials.gov whose main condition is Insomnia / Sleep Disorders: recruiting, active or completed, most recently updated first. Data retrieved 2026-10-28.
People with opioid use disorder (OUD) can have trouble falling or staying asleep. Researchers want to know if suvorexant will help people with OUD fall asleep and stay asleep. The goal of this study is to learn about the safety of suvorexant and how well people tolerate it. Researchers also want to ...
The purpose of this study is to assess the relative effectiveness, safety, and durability of the most commonly used prescription (zolpidem, trazodone) and over-the-counter (OTC) (melatonin, diphenhydramine) medications for insomnia, as well as a less commonly used prescription that may have a better...
The purpose of this study is to evaluate the efficacy of APSTZD compared to one active drug and placebo in insomnia treatment.
This study tests the efficacy of cognitive behavioural therapy for insomnia (CBT-I) with or without adjunct melatonin in older adults with insomnia. Adults aged 60 or above with chronic insomnia will be randomly assigned to one of three groups: (1) CBT-I plus nightly melatonin, (2) CBT-I plus nightl...
This study aims to evaluate the clinical effectiveness of Traditional Chinese Medicine (TCM) in treating sleep disorders, specifically chronic insomnia. While conventional TCM treatments often rely heavily on subjective patient feedback, this clinical trial incorporates objective diagnostic tools, i...
This is a randomized, double-blinded, placebo-controlled clinical trial. Eligible participants will randomized into either treatment group (CM granules) or placebo group (placebo granules) for 6 weeks, followed by a post-treatment visit at week 9. The primary outcome is the change in Pittsburgh Slee...
The study is a parallel group, double blind, randomized trial. Subjects will be recruited from individuals undergoing elective surgery for orthopedic, abdominal, urologic, gynecologic or spine reasons. Out of 92 subjects, one experimental group of 46 subjects will receive 20 mg Suvorexant beginning ...
The purpose of this study is to evaluate the clinical and cost-effectiveness of an intelligent therapy based on digital cognitive behavioral therapy for insomnia disorders
The main purpose of this study is to assess efficacy and safety of YZJ-1139 in adult subjects with insomnia disorder. Efficacy will be evaluated on objective and subjective sleep parameters.
Primary Objective : To evaluate the effect of ticagrelor tablets on the pharmacokinetic characteristics of YZJ-1139 in healthy subjects; Secondary Objective: To evaluate the safety of ticagrelor tablets in combination with YZJ-1139 tablets in healthy subjects.
Objective: 1. To evaluate the pharmacokinetics of YZJ-1139 tablets in patients with severe renal impairment and in subjects with normal renal impairment. 2. To evaluate the safety of YZJ-1139 tablets in patients with severe renal impairment and in subjects with normal renal impairment.
Insomnia is a common sleep disorder in which a person has difficulty falling asleep or staying asleep or getting good quality sleep. Consequences of insomnia include daytime sleepiness, poor memory function, decline in concentration with negative impacts on social and work activities. Although medic...
The main purpose of this study is to assess efficacy of YZJ-1139 for 28 days in adult subjects with insomnia disorder. Efficacy will be evaluated on objective and subjective sleep parameters.
This is a multicenter, double-blind, randomized study to evaluate the efficacy and safety of a daily single oral dose of tasimelteon and matching placebo in male and female pediatric participants with insomnia disorder.
Many Veterans with posttraumatic stress disorder (PTSD) have trouble sleeping or have frequent nightmares. So far, no medication has been approved for treatment of insomnia in PTSD. The purpose of this research study is to find out if taking medications called trazodone or eszopiclone can help decre...
Agents Found By Disease-Level Search
Searched directly from “Insomnia / Sleep Disorders” via ClinicalTrials.gov interventions and Open Targets' disease→drug data — independent of the 9-gene target panel above. This surfaces agents whose mechanism doesn't route through a curated gene (combination therapies, standard-of-care drugs, targets outside the panel).
35 agents shown (approved or with trial evidence) — 33 not found by the gene-target search above.
Suvorexant
Zolpidem
Internet-delivered CBT for InsomniaNOT in gene-target list
Internet-delivered CBT for Pain ManagementNOT in gene-target list
GabapentinNOT in gene-target list
Lemborexant 10 MGNOT in gene-target list
CBT for Menopausal Insomnia (CBTMI)NOT in gene-target list
TIAN WANG BU XIN DANNOT in gene-target list
Suan Tzao Ren TangNOT in gene-target list
Latin DanceNOT in gene-target list
CefalyNOT in gene-target list
CBTINOT in gene-target list
MRTINOT in gene-target list
Heart-rate variability biofeedback interventionNOT in gene-target list
SleepStyle 200 Auto Series with SensAwakeNOT in gene-target list
SleepStyle 200 Auto Series with out SensAwakeNOT in gene-target list
Xbox 360 KinectNOT in gene-target list
Night Time TeaNOT in gene-target list
Control TeaNOT in gene-target list
i-Sleep & BioClockNOT in gene-target list
SHUTiNOT in gene-target list
WELT-IPNOT in gene-target list
SHUTi (Sleep Health Using the Internet)NOT in gene-target list
Sleep ALL NightNOT in gene-target list
Food-Grown MagnesiumNOT in gene-target list
Microcrystalline celluloseNOT in gene-target list
GABANOT in gene-target list
In Person CBT-INOT in gene-target list
CBT-I via COASTNOT in gene-target list
Sleep OptimizationNOT in gene-target list
Stimulus Control TherapyNOT in gene-target list
Sleep Intervention for PTSD (SIP).NOT in gene-target list
Modified Suan ZaoRen Tang-TianWang BuXin DanNOT in gene-target list
Nightmare Deconstruction and ReprocessingNOT in gene-target list
NightWareNOT in gene-target list
Generated by the Open Source Medicine Foundation Biomarker Pipeline — 2026-10-08. Data sources: DGIdb, Open Targets, ChEMBL, PubMed, ClinicalTrials.gov. Not medical advice.