TRH [Ligand Id: 2139] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1472 (5-oxo-pro-his-pro-nh2, A-38579, ABBOTT-38579, Lopremone, NSC-760113, Protirelin, Protirelina, Protireline, Protirelin, synthetic, Protirelin tartrate, Relefact trh, Synthetic TRH, SYNTHETIC TRH, Thypinone, Thyrel trh, Thyroid releasing hormone, Thyroliberin, Thyrotropin-releasing factor, Thyrotropin releasing hormone, Thyrotropin-releasing hormone, Trh-cambridge) |
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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 | F | 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 | F | 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 | F | 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 | F | 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 | F | 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 | F | 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: A6IZR3] | ||||||||
| 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] |
| Translocator protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5742] [GtoPdb: 2879] [UniProtKB: P30536] | ||||||||
| ChEMBL | PDSP Secondary Binding target: TSPO - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5 | pKi | >10000 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
