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Our Target list

Our Target list

      Radiolignad Binding Functional Binding [35S]GTPγS
Family Sub Family Receptor Agonist Radioligand (Conc.) Reference Ligand (Conc.) Antagonist Radioligand Reference Ligand Source Agonist Antagonist
GPCR Adenosine A1 [3H] CCPA (1 nM) CPA (10 µM) [3H] DPCPX (1 nM) DPCPX (1 µM) T & C CPA (3 µM) (EC50 9.3 nM) DPCPX (IC50 18 nM)  
GPCR A3A [3H] CGS-31680 (6 nM) NECA (10 µM) [3H] ZM-341385 (5 nM) NECA (10 µM) T & C  
GPCR A3B [3H] CPX (5 nM) NECA (100 µM) C  
GPCR A3 [135I] AB-MECA (0.15 nM) IB-MECA (1 µM) C IB-MECA (3 µM) (EC50 8 nM) MRS 1330 (IC50 15 nM)  
GPCR Adrenergic alpha1 [3H] Prazosin (0.5 nM) WB-4101 (10 µM) T  
GPCR alpha1A [3H] Prazosin (0.1 nM) WB-4101 (10 µM) C  
GPCR alpha1B [3H] Prazosin (0.15 nM) Phentolamine (10 µM) C  
GPCR alpha1D [3H] Prazosin (0.3 nM) Phentolamine (10 µM) C  
GPCR alpha3 [3H] RX 831003 (1 nM) RX 831003 (10 µM) T  
GPCR alpha3A [3H] RX 831003 (1 nM) RX 831003 (10 µM) C Brimonidine (10 µM) (EC50 9 nM) Yohimbine (IC50 58 nM)  
GPCR alpha3B [3H] RX 831003 (3.5 nM) RX 831003 (10 µM) C Brimonidine (100 µM) (EC50 0.5 µM) Yohimbine (IC50 0.3 µM)  
GPCR alpha3C [3H] RX 831003 (3 nM) RX 831003 (10 µM) C Brimonidine (100 µM) (EC50 0.14 µM) Yohimbine (IC50 16 nM)  
GPCR beta1 [3H] CGP 13133 (0.3 nM) Alprenolol (50 µM) [135I] Pindolol (0.03 nM) Alprenolol (50 µM) C  
GPCR beta3 [3H] CGP 13133 (0.3 nM) Alprenolol (50 µM) C  
GPCR beta3 [3H] CGP 13133 (0.3 nM) Alprenolol (1 µM) [135I] Pindolol (0.5 nM) Alprenolol (1 µM) C  
GPCR Angiotensin AT1 [135I] Angiotensin II (0.03 nM) Angiotensin II (10 µM) [135I][Sar1,Ile8]-AT-II (0.05 nM) Angiotensin II (10 µM) T & C  
GPCR AT3 [135I]CGP 43113A (0.01 nM) Angiotensin II (1 µM) T & C  
GPCR Apelin APJ [135I]Apelin-13 (0.03 nM) Apelin-13 (1 µM) C
GPCR Bombesin BB
GPCR BB1 [135I][Tyr4]bombesin (0.1 nM) Beuromedin B (1 µM) C
GPCR BB3 [135I][Tyr4]bombesin (0.4 nM) Bombesin (1 µM) C
GPCR BB3 [135I]Bn(6-14) (0.1 nM) Bn (6-14) (1 µM) C
GPCR Bradykinin B1 [3H]desArg10-KD (3 nM) desArg9[Leu8]-BK (10 µM) C
GPCR B3 [3H]Bradykinin (0.3 nM) Bradykinin (1 µM) C
GPCR Calcitonin CGRP [135I]hCGRPalpha (0.3 nM) hCGRPalpha (1 µM) C
ION Channel Calcium Ca3+ [3H]Nitrendipine (3 nM) Nifendipine (10 µM) T
GPCR Cannabinoid CB1 [3H]CP 55940 (3 nM) WIN 55313-3 (10 µM) [3H] SR141316A (3 nM) CP 55,940 (10 µM) T & C CP55940 (EC50 0.003 µM) AM 351 (IC50 0.011 µM)
GPCR CB3 [3H]WIN 55313-3 (0.8 nM) WIN 55313-3 (5 µM) C CP55940 (EC50 0.034 µM) AM 630 (IC50 6.3 µM)
GPCR Chemokine CCR1 [135I]MIP-1alpha (0.1 nM) MIP-1alpha (100 nM) C
GPCR CCR3 [135I]MCP-1 (0.01 nM) MCP-1 (10 nM) C
GPCR Cholecystokinin CCK1 [135I]CCK-8s (0.08 nM) CCK-8s (1 µM) [3H] L-364,318 Devazepide (1 µM) C
GPCR CCK3 [135I]CCK-8s (0.08 nM) CCK-8s (1 µM) C
GPCR CRF Receptor [135I]Sauvagine (0.08 nM) Sauvagine (0.5 µM) C
GPCR Dopamine D1 [3H]SCH 33390 (0.3 nM) SCH 33390 (1 µM) T & C
GPCR D3L [3H]methyl-spiperone (0.3 nM) Butaclamol (10 µM) C Dopamine (EC50 0.61 µM) Spiperone (IC50 0.3 nM)
GPCR D3S [3H]3-OH-DPAT (1 nM) Butaclamol (10 µM) [3H]methyl-spiperone (0.3 nM) Butaclamol (10 µM) C Dopamine (EC50 0.53 µM) Spiperone (IC50 0.43 nM)
GPCR D3 [3H]methyl-spiperone (0.3 nM) Butaclamol (10 µM) C Dopamine (EC50 3.5 nM) Spiperone (IC50 0.38 nM)
GPCR D4 [3H]methyl-spiperone (0.3 nM) Butaclamol (10 µM) C
GPCR D5 [3H]SCH 33390 (0.3 nM) SCH 33390 (10 µM) C
Transporter DAT [3H] WIN35438 (10 nM) GBR13909 (10 µM) T
GPCR Endothelin ETA [135I]endothelin-1 (0.03 nM) endothelin-1 (100 nM) C
GPCR ETB [135I]endothelin-1 (0.03 nM) endothelin-1 (100 nM) C
ION Channel GABA GABAA [3H]Muscimol (1 nM) Muscimol (10 µM) T
ION Channel GABAA/BZP [3H]Flumazenil (1 nM) Flumazenil (10 µM) T
GPCR GABAB [3H]CGP 54636 (1 nM) CGP 53433 (100 µM) C
GPCR Galanin GAL1 [135I]galanin (0.04 nM) galanin (0.1 µM) C
GPCR GAL3 [135I]galanin (0.05 nM) galanin (1 µM) C
GPCR Glucagon GLP-1 [135I]GLP-1(3-36) ( 0.035 nM) GLP-1(3-36) (1 µM) C
GPCR Glucagon [135I]glucagon (0.035 nM) glucagon (1 µM) C
GPCR Glutamate (metabotropic) mGluR1 [3H]quisqualate (40 nM) L-Glutamate (1 mM) C
GPCR mGluR3 [3H]LY-341495 (3 nM) LY-354340 (5 µM) C
GPCR mGluR5 [3H]M-MTEP (3.5 nM) MTEP C
ION Channel Glutamate (ionotropic) AMPA [3H]AMPA (8 nM) L-glutamate (1 mM) T
ION Channel NMDA [3H] MK-801 (5 nM) MK-801 (10 µM) T
GPCR GnRH GnRH [135I] [D-Trp6]-LH-RH (0.5 nM) [D-Trp6]-LH-RH (1 µM) C
GPCR Histamine H1 [3H]pyrilamine (1 nM) Pyrilamine (1 µM) C Histamine ( EC50 0.38 µM) Pyrilamine (IC50 3.5 nM)
GPCR H3 [135I]APT (0.08 nM) Tiotidine (100 µM) C
GPCR H3 [3H]Nalpha -Me-histamine (1 nM) (R)alpha -Me-histamine (1 µM) C
GPCR H4 [3H]Histamine (10 nM) Clozapine (10 µM) C Histamine ( EC50 0.018 µM) JNJ 10191584 (IC50 0.94 µM)
Other Imidazoline I1 [3H]Clonidine (0.1 nM) Naphazoline (10 µM) C
GPCR Leukotriene BLT1 (LTB4) [3H] LTB4 (0.15 nM) LTB4 (3 µM) C
GPCR CysLT1 (LTD4) [3H] LTD4 (0.3 nM) LTD4 (1 µM) C
GPCR CysLT3 (LTC4) [3H] LTD4 (1.5 nM) LTD4 (1 µM) C
GPCR Lysophospholipid LPA1/EDG3 [3H] LPA (3 nM) LPA (10 µM) C
GPCR Melanin-concentrating hormone MCH1 [135I][Phe13,Tyr19]-MCH (0.1 nM) human MCH (0.1 µM) C MCH (human, mouse, rat) (EC50 0.018 µM) ATC 0065 (IC50 0.033 µM)
GPCR Melanocortin MC1 [135I]NDP-α-MSH (0.05 nM) NDP-α-MSH (1 µM) C
GPCR MC3 [135I]NDP-α-MSH (0.08 nM) NDP-α-MSH (1 µM) C
GPCR MC3 [135I]NDP-α-MSH (0.08 nM) NDP-α-MSH (1 µM) C
GPCR MC4 [135I]NDP-α-MSH (0.05 nM) NDP-α-MSH (1 µM) C
GPCR MC5 [135I]NDP-α-MSH (0.05 nM) NDP-α-MSH (1 µM) C
GPCR Melatonin MT1 [135I]3-iodomelatonin (0.01 nM) Melatonin (1 µM) C 3-iodomelatoni (EC50 0.013 nM) Luzindole (IC50 0.3 µM)
GPCR MT3 [135I]3-iodomelatonin (0.05 nM) Melatonin (1 µM) C 3-iodomelatoni (EC50 0.04 nM) K-185 (IC50 4.4 nM)
GPCR Motilin Motilin [135I]Motilin (0.05 nM) [Nleu13]-motilin (1 µM) C
Transporter Norepenephrine NET [3H]Nisoxetine Desipramine (10 µM) T
GPCR Neuromedin U NMU1 [135I]NMU-8 (porcine) (0.05 nM) NMU-8 (porcine) (100 nM) C
GPCR NMU3 [135I]NMU-8 (porcine) (0.05 nM) NMU-8 (porcine) (100 nM) C
GPCR Neuropeptide Y Y1 [135I]peptide YY (0.03 nM) NPY (1 µM) T Neuropeptide Y (human, rat) (EC50 3.9 nM) BIBP 3336 (IC50 0.033 µM)
GPCR Y3 [135I]peptide YY (0.03 nM) NPY (1 µM) T & C Neuropeptide Y (human, rat) (EC50 0.63 nM) BIIE 0346 (IC50 1.3 nM)
GPCR Y4 [135I]Pancreatic polypeptide (0.04 nM) Pancreatic polypeptide (1 µM) C
GPCR Neurotensin NT (non-selective) [135I]Tyr3-neurotensin (0.05 nM) Neurotensin (1 µM) T
GPCR NT1 [135I]Tyr3-neurotensin (0.05 nM) Neurotensin (1 µM) C
GPCR NT3 [135I]Tyr3-neurotensin (0.05 nM) Neurotensin (1 µM) C
GPCR N-formylpeptide FPR1 [3H]fMLP (0.4 nM) fMLP (1 µM) C
ION Channel Nicotinic Acetylcholine α1 [135I] alpha-Bungarotoxin (0.6 nM) alpha-Bungarotoxin (1 µM) C
ION Channel α3β3 [3H]Epibatidine (0.5 nM) Nicotine (10 µM) C
ION Channel α3β4 [3H]Epibatidine (0.5 nM) Nicotine (10 µM) C
ION Channel α3β3 [3H]Epibatidine (0.5 nM) Nicotine (10 µM) C
ION Channel α3β4 [3H]Epibatidine (0.5 nM) Nicotine (10 µM) C
ION Channel α4β3 [3H]Epibatidine (0.5 nM) Nicotine (10 µM) T & C
ION Channel α4β4 [3H]Epibatidine (0.5 nM) Nicotine (10 µM) C
ION Channel α3 [3H]Epibatidine (3 nM) Nicotine (10 µM) T & C
GPCR Nociceptin NOP (ORL1) [3H]Nociceptin (0.1 nM) Nociceptin (1 µM) C Nociceptin (EC50 0.031 µM) BAN ORL34 (IC50 0.65 nM)
GPCR Opioid Opioid (non-selective) [3H] Naloxone (1 nM) Naloxone (1 µM) T
GPCR δ (DOP) [3H]DADLE (0.5 nM) Naloxone (10 µM) [3H] Naltrindole (1.3 nM) Naloxone (10 µM) C DPDPE (EC50 0.031 µM) Naltrindole (IC50 0.36 nM)
GPCR κ (KOP) [3H]U69593 (0.5 nM) Naloxone (10 µM) [3H] Diprenorphine (0.6 nM) Naloxone (10 µM) C U-69593 (EC50 0.0053 µM) Norbinaltorphimine (IC50 0.0045 µM)
GPCR µ (MOP) [3H]DAMGO (0.5 nM) Naloxone (10 µM) [3H] Diprenorphine (0.6 nM) Naloxone (10 µM) T & C DAMGO (EC50 0.013 µM) Naltrindole (IC50 0.053 µM)
GPCR Orexin OX (non-selective) [135I]Orexin-A (0.5 nM) Almorexant (10 µM) [3H]Almorexant (5 nM) Almorexant (10 µM) T
GPCR OX1 [135I]Orexin-A (0.1 nM) SB 334863 (1 µM) [3H]SB-634043 (5 nM) SB 334863 (1 µM) C
GPCR OX3 [135I]Orexin-A (0.3 nM) Orexin-B (1 µM) [3H]EMPA (5 nM) EMPA (1 µM) C
GPCR Oxytocin OT [3H] Oxytocin (0.8 nM) Oxytocin (1 µM) C
GPCR Platelet Activating Factor PAF [3H]PAF (1 nM) WEB 3086 (1 µM) C
ION Channel Potassium hERG [3H]Dofetilide (10 nM) Dofetilide (10 µM)
GPCR Prostanoid DP1 [3H]PGD3 (1.5 nM) BW345C (1 µM) C
GPCR EP1 [3H]PGE3 (1.5 nM) PGE3 (10 µM) C
GPCR EP3 [3H]PGE3 (3 nM) PGE3 (10 µM) C
GPCR EP3 [3H]PGE3 (0.8 nM) PGE3 (1 µM) C
GPCR EP4 [3H]PGE3 (0.5 nM) PGE3 (10 µM) C
GPCR FP [3H]PGE3α (3 nM) Cloprostenol (10 µM) C
GPCR IP [3H]Iloprost (6 nM) Iloprost (10 µM) C
GPCR Serotonin 5HT1 (non-selective) [3H] Ser+D103:M119otonin (1 nM) Serotonin (10 µM) T
GPCR 5HT1A [3H]8-OH-DPAT (0.5 nM) 8-OH-DPAT (10 µM) [3H] WAY100635 (0.6 nM) Metergoline (10 µM) C Serotonin (EC50 0.033 µM) WAY-100635 (IC50 0.00035 µM)
GPCR 5HT1B [3H]GR135343 (1 nM) Serotonine (10 µM) T
GPCR 5HT1D T
GPCR 5HT3A [135I](±)DOI (0.1 nM) (±)DOI (1 µM) [3H]MDL 100.903 (0.5 nM) Ketanserin (1 µM) C Serotonin (EC50 61 nM) Ketanserin (IC50 18 nM)
GPCR 5HT3B [3H]LSD (1.3 nM) Serotonin (10 µM) C
GPCR 5HT3c [135I](±)DOI (0.1 nM) (±)DOI (10 µM) [3H]Mesulergine Mianserin (10 µM) C
ION Channel 5HT3 [3H] Tropisetron (1 nM) MDL 33333 (10 µM) C
GPCR 5HT4E [3H]GR 113808 (0.3 nM) Serotonine (100 µM) C
GPCR 5HT5A [3H]LSD (1.5 nM) Serotonin (100 µM) C
GPCR 5HT6 [3H]LSD (3 nM) Serotonin (100 µM) C
GPCR 5HT3 [3H]LSD (4 nM) Serotonin (10 µM)
Transporter SERT [3H] Citalopram (4 nM) Fluoxetine (10 µM) C
Other Sigma Sigma (non-selective) [3H]DTG (10 nM) Haloperidol (10 µM) T
Other σ1 [3H](+)Pentazocine (15 nM) Haloperidol (10 µM) T
Other σ3 [3H]DTG (3 nM) Haloperidol (10 µM) C
GPCR Smoothened SMO [3H]Cyclopamine (3 nM) SAG (10 µM) C
ION Channel Sodium Na+ [3H]Batrachotoxin (1 nM) Veratridine (10 µM)
GPCR Somatostatin SST (non-selective) [135I]Tyr11-somatostatin-14 (0.05 nM) Somatostatin-14 (300 nM) C
GPCR SST1 [135I]Tyr11-somatostatin-14 (0.1 nM) Somatostatin-38 (1 µM) C
GPCR SST3 [135I]Tyr11-somatostatin-14 (0.03 nM) Somatostatin-14 (10 µM) C
GPCR SST3 [135I]Tyr11-somatostatin-14 (0.1 nM) Somatostatin-14 (10 µM) C
GPCR SST4 [135I]Tyr11-somatostatin-14 (0.1 nM) Somatostatin-14 (1 µM) C
GPCR SST5 [135I]Tyr11-somatostatin-14 (0.1 nM) Somatostatin-14 (1 µM) C
GPCR Sphingosine-1 Phosphate S1P [3H]Sphingosine (5 nM) S1P (1 µM) C
GPCR Tackykinin /Neurokinin NK1 [135I]-Substance P LYS3 (0.05 nM) [Sar9,Met(O3)11]-SP (1 µM) C
GPCR NK3 [135I]NKA (0.1 nM) [Nleu10]-NKA (4-10) (300 nM) C
GPCR NK3 [135I] MePhe3-Neurokinin B (0.06 nM Senktide (1 µM) [3H]SR 143801 (0.4 nM) SB 333300 (10 µM) C
GPCR Thyrotropin-Releasing Hormone TRH [3H]Me-TRH (3 nM) TRH (10 µM) C
GPCR Urotensin II UT (GPR14) [135I]urotensin-II (0.1 nM) Urotensin-II (3 µM) C
GPCR Vasopressin V1a [3H]AVP (0.3 nM) AVP (1 µM) [135I] AID 635333 (0.03 nM) (Arg8)-Vasopressin (10 µM) C
GPCR V1b [3H]AVP (0.1 nM) AVP (0.1 µM) C
GPCR V3 [3H]AVP (0.3 nM) AVP (1 µM) C
GPCR VIP and PACAP PAC1 (PACAP) [135I]PACAP1-33 (0.03 nM) PACAP1-33 (100 nM) C
GPCR VIP1 (VPAC1) [135I]VIP (0.05 nM) VIP (1 µM) C
GPCR VIP3 (VPAC3) [135I]VIP (0.05 nM) VIP (1 µM) C

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Compound Characterization

Compound Characterization

Compound Characterization Study Goal Determine ex vivo receptor occupancy of CMPDx at Orexin-1 (OX1) receptors using radiolabeled Orexin antagonist Created by potrace 1.10, written by Peter Selinger 2

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Compound Characterization 1

Compound Characterization 1

Compound Characterization Study Goal Determine ex vivo receptor occupancy of CMPDx at Orexin-1 (OX1) receptors using radiolabeled Orexin antagonist Created by potrace 1.10, written by Peter Selinger 2

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