ChEMBL ligand: CHEMBL14453
MT1 receptor/Melatonin receptor 1A in Human [ChEMBL: CHEMBL1945] [GtoPdb: 287] [UniProtKB: P48039] There should be some charts here, you may need to enable JavaScript!
MT2 receptor/Melatonin receptor 1B in Human [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286] 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
MT1 receptor/Melatonin receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1945] [GtoPdb: 287] [UniProtKB: P48039]
ChEMBL	Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells	B	8.51	pKi	3.1	nM	Ki	J Med Chem (2014) 57: 3161-3185 [PMID:24228714]
GtoPdb	-	-	9.2	pKi	-	-	-	Naunyn Schmiedebergs Arch Pharmacol (2003) 367: 553-61 [PMID:12764576]
ChEMBL	Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand	B	9.22	pKi	0.6	nM	Ki	J Med Chem (2003) 46: 1127-1129 [PMID:12646022]
ChEMBL	Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells	B	9.22	pKi	0.6	nM	Ki	Bioorg Med Chem (2010) 18: 3426-3436 [PMID:20444610]
ChEMBL	Binding affinity to MT1 receptor (unknown origin) expressed in HEK cells	B	9.22	pKi	0.6	nM	Ki	J Med Chem (2014) 57: 3161-3185 [PMID:24228714]
ChEMBL	Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 mins	B	9.22	pKi	0.6	nM	Ki	Medchemcomm (2015) 6: 1340-1344
ChEMBL	Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay	F	7.14	pEC50	73	nM	EC50	Bioorg Med Chem (2010) 18: 3426-3436 [PMID:20444610]
MT2 receptor/Melatonin receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286]
ChEMBL	Displacement of [125I]2-iodomelatonin from human MT2 receptor expressed in CHO cells	B	6.78	pKi	167	nM	Ki	J Med Chem (2014) 57: 3161-3185 [PMID:24228714]
ChEMBL	Binding affinity to MT2 receptor (unknown origin) expressed in HEK cells	B	7.14	pKi	73.2	nM	Ki	J Med Chem (2014) 57: 3161-3185 [PMID:24228714]
ChEMBL	Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT2 expressed in HEK293 cells after 120 mins	B	7.14	pKi	73.2	nM	Ki	Medchemcomm (2015) 6: 1340-1344
ChEMBL	Binding affinity for human Melatonin receptor type 1B stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand	B	7.14	pKi	72.7	nM	Ki	J Med Chem (2003) 46: 1127-1129 [PMID:12646022]
ChEMBL	Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells	B	7.14	pKi	72.7	nM	Ki	Bioorg Med Chem (2010) 18: 3426-3436 [PMID:20444610]
GtoPdb	-	-	7.2	pKi	-	-	-	Naunyn Schmiedebergs Arch Pharmacol (2003) 367: 553-61 [PMID:12764576]
ChEMBL	Agonist activity at human MT2 receptor expressed in CHO cells by [35S]GTPgamma binding assay	F	6.39	pEC50	405	nM	EC50	Bioorg Med Chem (2010) 18: 3426-3436 [PMID:20444610]

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]