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Phase I
Phase II
Phase III
Phase IV
Untapped targets
Sensory



A5-HT1A5-HT1B5-HT1D5-HT1E5-HT1F5-HT2A5-HT2B5-HT2C5-HT45-HT5A5-HT65-HT7M1M2M3M4M5A1A2AA2BA3α1Aα1Bα1Dα2Aα2Bα2Cβ1β2β3AT1AT2ApelinGPBABB1BB2BB3B1B2CB1CB2ChemerinChemerin 2CCR1CCR2CCR3CCR4CCR5CCR6CCR7CCR8CCR9CCR10CXCR1CXCR2CXCR3CXCR4CXCR5CXCR6CX3CR1XCR1ACKR1ACKR2ACKR3ACKR4CCRL2CCK1CCK2C3aC5a1C5a2D1D2D3D4D5ETAETBGPERFPR1FPR2/ALXFPR3FFA1FFA2FFA3FFA4GPR42GAL1GAL2GAL3GhrelinFSHLHTSHGnRH1GPR18GPR55GPR119H1H2H3H4HCA1HCA2HCA3KisspeptinBLT1BLT2CysLT1CysLT2OXELPA1LPA2LPA3LPA4LPA5LPA6S1P1S1P2S1P3S1P4S1P5MCH1MCH2MC1MC2MC3MC4MC5MT1MT2MotilinNMU1NMU2NPFF1NPFF2NPSNPBW1NPBW2Y1Y2Y4Y5Y6NTS1NTS2δκμNOPRhodopsinOPN3OPN4OPN5OPN1SWOPN1MWOPN1LWRRHOX1OX25-HTAcetylcholineAdenosineAdrenoceptorsAngiotensinApelinBile acidBombesinBradykininCannabinoidChemerinChemokineCholecystokininComplement peptideDopamineEndothelinEstrogenFormylpeptideFree fatty acidGalaninGhrelinGlycoprotein hormoneGonadotrophin-rel. hormoneGPR18, 55 & 119HistamineHydroxycarboxylic acidKisspeptinLeukotrieneLysophospholipidLysophospholipidMelanin-conc. hormoneMelanocortinMelatoninMotilinNeuromedin UNeuropeptide FF/AFNeuropeptide SNeuropeptide W/BNeuropeptide YNeurotensinOpioidOpsinsOrexinAOxoglutarateP2Y1P2Y2P2Y4P2Y6P2Y11P2Y12P2Y13P2Y14QRFPPAFPKR1PKR2PrRPDP1DP2EP1EP2EP3EP4FPIPTPPAR1PAR2PAR3PAR4RXFP1RXFP2RXFP3RXFP4SST1SST2SST3SST4SST5SuccinateNK1NK2NK3TRH1TA1UTV1AV1BV2OTGPR3GPR4GPR6GPR12GPR15GPR17GPR19GPR20GPR21GPR22GPR25GPR26GPR27GPR31GPR32GPR33GPR34GPR35GPR37GPR37L1GPR39GPR45GPR50GPR52GPR61GPR62GPR63GPR65GPR68GPR75GPR78GPR82GPR83GPR84GPR85GPR87GPR88GPR101GPR132GPR135GPR139GPR141GPR142GPR146GPR148GPR149GPR150GPR151GPR152GPR153GPR160GPR161GPR162GPR171GPR173GPR174GPR176GPR182GPR183LGR4LGR5LGR6MAS1MAS1LMRGPRDMRGPREMRGPRFMRGPRGMRGPRX1MRGPRX2MRGPRX3MRGPRX4P2RY8P2RY10TAAR2TAAR3TAAR5TAAR6TAAR8TAAR9OxoglutarateP2YPeptide P518Platelet-activating factorProkineticinProlactin-rel. peptideProstanoidProteinase-activatedRelaxin family peptideSomatostatinSuccinateTachykininThyrotropin-rel. hormoneTrace amineUrotensinVasopressin & oxytocinClass A orphansB1CTCalcitonin-likeCRF1CRF2GHRHGIPGLP-1GLP-2GlucagonSecretinPTH1PTH2PAC1VPAC1VPAC2B2ADGRA1ADGRA2ADGRA3ADGRB1ADGRB2ADGRB3CELSR1CELSR2CELSR3ADGRD1ADGRD2ADGRE1ADGRE2ADGRE3ADGRE4PADGRE5ADGRF1ADGRF2ADGRF3ADGRF4ADGRF5ADGRG1ADGRG2ADGRG3ADGRG4ADGRG5ADGRG6ADGRG7ADGRL1ADGRL2ADGRL3ADGRL4ADGRV1CalcitoninCorticotropin-rel. factorGlucagon familyParathyroid hormoneVIP & PACAPADGRAADGRBADGRCADGRDADGREADGRFADGRGADGRLADGRVCCaSGPR156GPR158GPR179GPRC5AGPRC5BGPRC5CGPRC5DGPRC6GABAB1GABAB2MGlu1MGlu2MGlu3MGlu4MGlu5MGlu6MGlu7MGlu8TAS1R1TAS1R2TAS1R3FFZD1FZD2FZD3FZD4FZD5FZD6FZD7FZD8FZD9FZD10SMOCalcium-sensingOrphansGABAMetabotropic glutamateTaste 1FrizzledT2TAS2R1TAS2R3TAS2R4TAS2R5TAS2R7TAS2R8TAS2R9TAS2R10TAS2R13TAS2R14TAS2R16TAS2R19TAS2R20TAS2R30TAS2R31TAS2R38TAS2R39TAS2R40TAS2R41TAS2R42TAS2R43TAS2R45TAS2R46TAS2R50TAS2R60ClasslessGPR107GPR137TPRA1GPR143GPR157

Receptor names:
Agent/drugs
New agents in trial

Repurposed drugs

Approved drugs
New agents in trial13015.5Repurposed drugs17940Approved drugs16734
Class AAminergic5-Hydroxytryptamine5HT1AApprovedRepurposedNew5HT1B5HT1D5HT1E5HT1F5HT2A5HT2B5HT2C5HT4R5HT6R5HT7RAcetylcholine ACM1ACM2ACM3ACM4ACM5AdrenoceptorsADA1AADA1BADA1DADA2AADA2BADA2CADRB1ADRB2ADRB3DopamineDRD1DRD2DRD3DRD4DRD5HistamineHRH1HRH2HRH3HRH4Trace amineTAAR1LipidCannabinoidCNR1CNR2Free fatty acidFFAR1LeukotrieneLT4R1LT4R2CLTR1CLTR2LysophospholipidLPAR1LysophospholipidS1PR1S1PR2S1PR3S1PR4S1PR5Platelet-activating factorPTAFRProstanoidPD2RPD2R2PE2R1PE2R2PE2R3PE2R4PF2RPI2RTA2RMelatoninMelatoninMTR1AMTR1BNucleotideAdenosineAA1RAA2ARAA2BRAA3RP2YP2RY1P2RY2P2RY4P2RY6P2Y12OrphanClass A orphansGPR6GPR52GPR84MASMRGX2MRGX4PeptideAngiotensinAGTR1AGTR2ApelinAPJBombesinGRPRBradykininBKRB2CholecystokininGASRComplement peptideC5AR1EndothelinEDNRAEDNRBGhrelinGHSRGonadotrophin-releasing hormoneGNRHRMelanocortinMSHRACTHRMC3RMC4RMC5RNeuropeptide YNPY2RNeurotensinNTR2OpioidOPRDOPRKOPRMOPRXOrexinOX1ROX2RProteinase-activatedPAR1PAR2Relaxin family peptideRXFP1RXFP2SomatostatinSSR1SSR2SSR3SSR4SSR5TachykininNK1RNK3RThyrotropin-releasing hormoneTRFRVasopressin and oxytocinV1ARV1BRV2ROXYRProteinChemokineCCR2CCR4CCR5CCR6CCR8CXCR1CXCR2CXCR3CXCR4CXCR5CX3C1ACKR3Glycoprotein hormoneFSHRLSHRTSHRClass B1PeptideCalcitoninCALCRCALRLCorticotropin-releasing factorCRFR1Glucagon receptor familyGHRHRGIPRGLP1RGLP2RGLRSCTRParathyroid hormonePTH1RPTH2RVIP and PACAPVIPR1VIPR2Class CAmino acidGABA BGABR1GABR2Metabotropic glutamateGRM2GRM3GRM5IonCalcium-sensingCASROrphanClass C OrphansGPC5DClass FProteinFrizzledSMO

Receptor names:
Clinical phases
Phase I

Phase II

Phase III

Phase IV
Phase I-III13417.5Phase IV16734
Class AAminergic5-Hydroxytryptamine5HT1APhase IVIIIIII5HT1B5HT1D5HT1E5HT1F5HT2A5HT2B5HT2C5HT4R5HT6R5HT7RAcetylcholine ACM1ACM2ACM3ACM4ACM5AdrenoceptorsADA1AADA1BADA1DADA2AADA2BADA2CADRB1ADRB2ADRB3DopamineDRD1DRD2DRD3DRD4DRD5HistamineHRH1HRH2HRH3HRH4Trace amineTAAR1LipidCannabinoidCNR1CNR2Free fatty acidFFAR1LeukotrieneLT4R1LT4R2CLTR1CLTR2LysophospholipidLPAR1LysophospholipidS1PR1S1PR2S1PR3S1PR4S1PR5Platelet-activating factorPTAFRProstanoidPD2RPD2R2PE2R1PE2R2PE2R3PE2R4PF2RPI2RTA2RMelatoninMelatoninMTR1AMTR1BNucleotideAdenosineAA1RAA2ARAA2BRAA3RP2YP2RY1P2RY2P2RY4P2RY6P2Y12OrphanClass A orphansGPR6GPR52GPR84MASMRGX2MRGX4PeptideAngiotensinAGTR1AGTR2ApelinAPJBombesinGRPRBradykininBKRB2CholecystokininGASRComplement peptideC5AR1EndothelinEDNRAEDNRBGhrelinGHSRGonadotrophin-releasing hormoneGNRHRMelanocortinMSHRACTHRMC3RMC4RMC5RNeuropeptide YNPY2RNeurotensinNTR2OpioidOPRDOPRKOPRMOPRXOrexinOX1ROX2RProteinase-activatedPAR1PAR2Relaxin family peptideRXFP1RXFP2SomatostatinSSR1SSR2SSR3SSR4SSR5TachykininNK1RNK3RThyrotropin-releasing hormoneTRFRVasopressin and oxytocinV1ARV1BRV2ROXYRProteinChemokineCCR2CCR4CCR5CCR6CCR8CXCR1CXCR2CXCR3CXCR4CXCR5CX3C1ACKR3Glycoprotein hormoneFSHRLSHRTSHRClass B1PeptideCalcitoninCALCRCALRLCorticotropin-releasing factorCRFR1Glucagon receptor familyGHRHRGIPRGLP1RGLP2RGLRSCTRParathyroid hormonePTH1RPTH2RVIP and PACAPVIPR1VIPR2Class CAmino acidGABA BGABR1GABR2Metabotropic glutamateGRM2GRM3GRM5IonCalcium-sensingCASROrphanClass C OrphansGPC5DClass FProteinFrizzledSMO