TRH [Ligand Id: 2139] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1472 (Protirelin, Lopremone, Protirelin tartrate, Thyrel trh, SYNTHETIC TRH, Thypinone, Trh-cambridge, Synthetic TRH, A-38579, ABBOTT-38579)
  • TRH1 receptor/Thyrotropin-releasing hormone receptor in Human [ChEMBL: CHEMBL1810] [GtoPdb: 363] [UniProtKB: P34981]
  • TRH1 receptor/Thyrotropin-releasing hormone receptor in Mouse [ChEMBL: CHEMBL2467] [GtoPdb: 363] [UniProtKB: P21761]
  • TRH1 receptor/Thyrotropin-releasing hormone receptor in Rat [ChEMBL: CHEMBL4553] [GtoPdb: 363] [UniProtKB: Q01717]
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  • Thyrotropin-releasing hormone receptor 2 in Mouse [ChEMBL: CHEMBL3600274] [UniProtKB: Q9ERT1]
  • Thyrotropin-releasing hormone receptor 2 in Rat [ChEMBL: CHEMBL3875] [UniProtKB: Q9R297]
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  • TRH2 receptor in Rat [GtoPdb: 754]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
TRH1 receptor/Thyrotropin-releasing hormone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1810] [GtoPdb: 363] [UniProtKB: P34981]
ChEMBL Displacement of [3H]N(1)-Me-His-TRH from TRHR1 B 7.7 pKi 20 nM Ki Bioorg. Med. Chem. (2007) 15: 433-443 [PMID:17035026]
ChEMBL Agonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity F 8.52 pEC50 3 nM EC50 Bioorg. Med. Chem. (2007) 15: 433-443 [PMID:17035026]
TRH1 receptor/Thyrotropin-releasing hormone receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2467] [GtoPdb: 363] [UniProtKB: P21761]
ChEMBL Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells. B 7.64 pKi 23 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 3093-3096 [PMID:9873682]
ChEMBL Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells B 8 pKi 10 nM Ki J. Med. Chem. (1996) 39: 1571-1574 [PMID:8648595]
ChEMBL Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs B 7.59 pIC50 26 nM IC50 Eur. J. Med. Chem. (2016) 111: 72-83 [PMID:26854379]
ChEMBL Displacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting method B 8.59 pIC50 2.6 nM IC50 Bioorg. Med. Chem. (2015) 23: 5641-5653 [PMID:26216015]
ChEMBL Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA B 8.49 pEC50 3.2 nM EC50 Eur. J. Med. Chem. (2016) 111: 72-83 [PMID:26854379]
ChEMBL Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method B 9 pEC50 1 nM EC50 Bioorg. Med. Chem. (2015) 23: 5641-5653 [PMID:26216015]
ChEMBL Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay B 9 pEC50 1 nM EC50 Eur. J. Med. Chem. (2016) 111: 72-83 [PMID:26854379]
ChEMBL Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells B 9.17 pEC50 0.68 nM EC50 J. Med. Chem. (1996) 39: 1571-1574 [PMID:8648595]
ChEMBL Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol B 9.31 pEC50 0.49 nM EC50 Bioorg. Med. Chem. Lett. (1998) 8: 3093-3096 [PMID:9873682]
TRH1 receptor/Thyrotropin-releasing hormone receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4553] [GtoPdb: 363] [UniProtKB: Q01717]
ChEMBL Inhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrain B 7.37 pKi 42.3 nM Ki J. Med. Chem. (2004) 47: 6025-6033 [PMID:15537357]
GtoPdb - - 7.4 pKi - - - Physiol Rev (1996) 76: 175-91 [PMID:8592728]
ChEMBL Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM B 7.7 pKi 20 nM Ki J. Med. Chem. (2005) 48: 6162-6165 [PMID:16162016]
ChEMBL Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uM B 8.52 pEC50 3 nM EC50 J. Med. Chem. (2005) 48: 6162-6165 [PMID:16162016]
Thyrotropin-releasing hormone receptor 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3600274] [UniProtKB: Q9ERT1]
ChEMBL Displacement of [3H]-1-MeHis-TRH from mouse TRH-R2 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting method B 8.15 pIC50 7 nM IC50 Bioorg. Med. Chem. (2015) 23: 5641-5653 [PMID:26216015]
ChEMBL Displacement of [3H]-Me-His-TRH from mouse TRH-R2 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs B 8.15 pIC50 7 nM IC50 Eur. J. Med. Chem. (2016) 111: 72-83 [PMID:26854379]
ChEMBL Agonist activity at mouse TRH-R2 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA B 8.51 pEC50 3.1 nM EC50 Eur. J. Med. Chem. (2016) 111: 72-83 [PMID:26854379]
ChEMBL Agonist activity at mouse TRH-R2 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method B 9.28 pEC50 0.52 nM EC50 Bioorg. Med. Chem. (2015) 23: 5641-5653 [PMID:26216015]
ChEMBL Agonist activity at mouse TRH-R2 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay B 9.3 pEC50 0.5 nM EC50 Eur. J. Med. Chem. (2016) 111: 72-83 [PMID:26854379]
Thyrotropin-releasing hormone receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3875] [UniProtKB: Q9R297]
ChEMBL Inhibitory constant against thyrotropin releasing hormone receptor 2 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH B 8 pKi 10 nM Ki J. Med. Chem. (2005) 48: 6162-6165 [PMID:16162016]
ChEMBL Displacement of [3H]N(1)-Me-His-TRH from TRHR2 B 8 pKi 10 nM Ki Bioorg. Med. Chem. (2007) 15: 433-443 [PMID:17035026]
ChEMBL Displacement of [3H]3-methylhistidyl-TRH from rat recombinant TRH2 receptor expressed in HEK2935 cells B 4.64 pIC50 23000 nM IC50 J. Nat. Prod. (2008) 71: 881-883 [PMID:18412395]
ChEMBL Displacement of [3H]3-methylhistidyl-TRH from rat recombinant TRHR2 expressed in HEK2935 cells B 7.64 pIC50 23 nM IC50 J. Nat. Prod. (2008) 71: 884-886 [PMID:18407692]
ChEMBL Signaling (activation) potency for thyrotropin releasing hormone receptor 2 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8 B 8.52 pEC50 3 nM EC50 J. Med. Chem. (2005) 48: 6162-6165 [PMID:16162016]
ChEMBL Agonist activity at TRHR2 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity F 8.52 pEC50 3 nM EC50 Bioorg. Med. Chem. (2007) 15: 433-443 [PMID:17035026]
TRH2 receptor in Rat [GtoPdb: 754]
GtoPdb - - 7.4 pKi - - - Physiol Rev (1996) 76: 175-91 [PMID:8592728]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]