Drug Targets
The CNS pipeline organized by molecular target — 92 targets across212 compound–target links, with the action, affinity, and development phase for each compound that acts on them.
- 5-HT2AHTR2A5-hydroxytryptamine receptor 2A24 compounds13 Phase 3+
- D2DRD2Dopamine D2 receptor11 compounds8 Phase 3+
- SERTSLC6A4Serotonin transporter10 compounds5 Phase 3+
- 5-HT1AHTR1A5-hydroxytryptamine receptor 1A9 compounds4 Phase 3+
- 5-HT2CHTR2C5-hydroxytryptamine receptor 2C9 compounds4 Phase 3+
- DATSLC6A3Dopamine transporter7 compounds4 Phase 3+
- NETSLC6A2Norepinephrine transporter7 compounds5 Phase 3+
- alpha-1A adrenoceptorADRA1AAlpha-1A adrenergic receptor5 compounds5 Phase 3+
- 5-HT2BHTR2B5-hydroxytryptamine receptor 2B4 compounds2 Phase 3+
- D3DRD3Dopamine D3 receptor4 compounds2 Phase 3+
- GluN2BGRIN2BGlutamate ionotropic receptor NMDA type subunit 2B4 compounds
- M1CHRM1Muscarinic acetylcholine receptor M14 compounds2 Phase 3+
- M4CHRM4Muscarinic acetylcholine receptor M44 compounds1 Phase 3+
- alpha7 nAChRCHRNA7Nicotinic acetylcholine receptor alpha7 subunit3 compounds1 Phase 3+
- GABA-A receptorGamma-aminobutyric acid type A receptor3 compounds1 Phase 3+
- KOROPRK1Kappa opioid receptor3 compounds
- NMDA receptorGRIN1Glutamate ionotropic receptor NMDA type3 compounds1 Phase 3+
- OX2RHCRTR2Orexin receptor type 2 (hypocretin receptor 2)3 compounds3 Phase 3+
- TAAR1Trace amine-associated receptor 13 compounds2 Phase 3+
- Tau (pT217)MAPTMicrotubule-associated protein tau, phosphorylated at threonine-217 (proline-rich domain)3 compounds
- V1a receptorAVPR1AArginine vasopressin receptor 1A3 compounds
- 5-HT7HTR75-hydroxytryptamine receptor 72 compounds2 Phase 3+
- CB1CNR1Cannabinoid receptor 12 compounds
- D1 receptorDRD1Dopamine D1 receptor2 compounds2 Phase 3+
- D4DRD4Dopamine D4 receptor2 compounds1 Phase 3+
- D5 receptorDRD5Dopamine D5 receptor2 compounds2 Phase 3+
- H1 receptorHRH1Histamine H1 receptor2 compounds2 Phase 3+
- H3 receptorHRH3Histamine H3 receptor2 compounds
- Kv7.2KCNQ2Potassium voltage-gated channel subfamily Q member 22 compounds2 Phase 3+
- Kv7.3KCNQ3Potassium voltage-gated channel subfamily Q member 32 compounds2 Phase 3+
- MOROPRM1Mu opioid receptor2 compounds
- Norepinephrine transporter (NET)SLC6A2Sodium-dependent noradrenaline transporter2 compounds2 Phase 3+
- OX2 receptorHCRTR2Orexin receptor type 2 (hypocretin receptor 2)2 compounds1 Phase 3+
- Oxytocin receptorOXTROxytocin receptor2 compounds
- Serotonin transporter (SERT)SLC6A4Sodium-dependent serotonin transporter2 compounds2 Phase 3+
- V1B receptorAVPR1BArginine vasopressin receptor 1B2 compounds
- 5-HT3 receptorHTR3A5-hydroxytryptamine receptor 31 compound
- alpha-2A adrenoceptorADRA2AAlpha-2A adrenergic receptor1 compound1 Phase 3+
- alpha-2B adrenoceptorADRA2BAlpha-2B adrenergic receptor1 compound1 Phase 3+
- alpha-2C adrenoceptorADRA2CAlpha-2C adrenergic receptor1 compound1 Phase 3+
- Alpha-synucleinSNCAAlpha-synuclein1 compound
- alpha3beta4 nAChRCHRNA3Neuronal nicotinic acetylcholine receptor alpha3beta4 subtype (CHRNA3/CHRNB4 heteropentamer), ganglionic1 compound
- alpha4beta2 nAChRCHRNA4Neuronal nicotinic acetylcholine receptor alpha4beta2 subtype (CHRNA4/CHRNB2 heteropentamer)1 compound
- AMPA receptorAlpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (ionotropic glutamate receptor, AMPA subtype)1 compound
- AMPA receptor (GluA1)GRIA1Glutamate ionotropic receptor AMPA type subunit 11 compound1 Phase 3+
- DAAODAOD-amino acid oxidase1 compound
- delta-opioid receptorOPRD1delta-type opioid receptor (DOP)1 compound1 Phase 3+
- DOROPRD1Delta-type opioid receptor1 compound
- EAAT2SLC1A2Excitatory amino acid transporter 2 (glial high-affinity glutamate transporter, GLT-1)1 compound
- FUSFused in sarcoma / RNA-binding protein FUS1 compound1 Phase 3+
- GABA-A receptor alpha-1GABRA1Gamma-aminobutyric acid type A receptor subunit alpha-11 compound
- GABA-A receptor alpha-2GABRA2Gamma-aminobutyric acid type A receptor subunit alpha-21 compound
- GABA-A receptor alpha-3GABRA3Gamma-aminobutyric acid type A receptor subunit alpha-31 compound
- GABA-A receptor alpha-5GABRA5Gamma-aminobutyric acid type A receptor subunit alpha-51 compound
- GABA-B receptorGABBR1Gamma-aminobutyric acid type B receptor subunit 1 (GABAB1)1 compound1 Phase 3+
- GHB receptorGHBRGamma-hydroxybutyrate (GHB) receptor1 compound1 Phase 3+
- GluN2AGRIN2AGlutamate ionotropic receptor NMDA type subunit 2A1 compound
- GluN2DGRIN2DGlutamate ionotropic receptor NMDA type subunit 2D1 compound
- GlyT1SLC6A9Sodium- and chloride-dependent glycine transporter 11 compound
- JAK1Tyrosine-protein kinase JAK11 compound
- kappa-opioid receptorOPRK1kappa-type opioid receptor (KOP)1 compound1 Phase 3+
- KAT-IIAADATKynurenine aminotransferase II (kynurenine/alpha-aminoadipate aminotransferase, mitochondrial)1 compound
- KgpkgpLysine-specific gingipain (lysine-gingipain, Porphyromonas gingivalis)1 compound
- LRP1Low-density lipoprotein receptor-related protein 11 compound
- Lysine-gingipain (Kgp)Lysine-specific gingipain, a cysteine protease virulence factor of Porphyromonas gingivalis1 compound
- mGlu2GRM2Metabotropic glutamate receptor 21 compound
- mGlu3GRM3Metabotropic glutamate receptor 31 compound
- mGluR2GRM2Metabotropic glutamate receptor 21 compound
- MT1MTNR1AMelatonin receptor 1A1 compound
- MT2MTNR1BMelatonin receptor 1B1 compound
- mTORC1MTORMechanistic target of rapamycin complex 11 compound
- mu-opioid receptorOPRM1mu-type opioid receptor (MOP)1 compound1 Phase 3+
- Nasal chemosensory neuron receptor (uncharacterized)Nasal chemosensory neuron receptor mediating olfactory-amygdala modulation (uncharacterized)1 compound
- Nasal chemosensory receptor neuronsPeripheral nasal chemosensory (olfactory/vomeronasal) receptor neurons1 compound1 Phase 3+
- OX1RHCRTR1Orexin receptor type 1 (OX1)1 compound1 Phase 3+
- PDE10AcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A1 compound
- PDE1ACalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A1 compound
- PDE1BCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B1 compound
- PDE1CCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C1 compound
- Phosphodiesterase 4PDE4cAMP-specific 3',5'-cyclic phosphodiesterase 41 compound
- Presynaptic glutamate release (voltage-gated Na+ channels)Voltage-gated sodium channels / presynaptic glutamate release machinery1 compound
- Sestrin2SESN2Sestrin-2 (leucine sensor)1 compound
- Sigma-1 receptorSIGMAR1Sigma non-opioid intracellular receptor 11 compound1 Phase 3+
- sigma-2 receptorTMEM97Sigma-2 receptor (TMEM97 / transmembrane protein 97)1 compound1 Phase 3+
- SIRT6NAD-dependent protein deacetylase sirtuin-61 compound
- TLXNR2E1Nuclear receptor TLX (tailless homolog, NR2E1)1 compound
- TRbetaTHRBThyroid hormone receptor beta1 compound
- TRPC4Short transient receptor potential channel 4 (transient receptor potential cation channel subfamily C member 4)1 compound
- TRPC5Short transient receptor potential channel 5 (transient receptor potential cation channel subfamily C member 5)1 compound
- TRPM3Transient receptor potential cation channel subfamily M member 31 compound
- TYK2Non-receptor tyrosine-protein kinase TYK21 compound
- VMAT2SLC18A2Vesicular monoamine transporter 21 compound