ChEMBL ligand: CHEMBL1472 (5-oxo-pro-his-pro-nh2, A-38579, ABBOTT-38579, Lopremone, NSC-760113, Protirelin, 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)
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] There should be some charts here, you may need to enable JavaScript!
Thyrotropin-releasing hormone receptor 2 in Mouse [ChEMBL: CHEMBL3600274] [UniProtKB: Q9ERT1] Thyrotropin-releasing hormone receptor 2 in Rat [ChEMBL: CHEMBL3875] [UniProtKB: Q9R297] There should be some charts here, you may need to enable JavaScript!
TRH2 receptor in Rat [GtoPdb: 754] There should be some charts here, you may need to enable JavaScript!

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: 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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]