Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T97613 Target Info
Target Name Melatonin receptor type 1A (MTNR1A)
Synonyms
Mel1a receptor; Mel1AR; Mel-1A-R
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Target Type Successful Target
Gene Name MTNR1A
Biochemical Class GPCR rhodopsin
UniProt ID
MTR1A_HUMAN
Co-Targets of This Target  Top
Co-Target Name Melatonin receptor type 1B (MTNR1B) Successful Target
UniProt ID MTR1B_HUMAN
Gene Name MTNR1B
Synonyms
Mel1b receptor; Mel1b melatonin receptor; Mel-1B-R
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Representative Drug(s) LY-156735 Drug Info Ki = 0.03981 nM Click to Show More [1]
2 Ramelteon Drug Info Ki = 0.045 nM [2]
3 Melatonin Drug Info EC50 = 0.069 nM [3]
Co-Target Name Quinone reductase 2 (NQO2) Successful Target
UniProt ID NQO2_HUMAN
Gene Name NQO2
Synonyms
Quinone oxidoreductase 2; Qui reductase 2; QR2; NRH:quinone oxidoreductase 2; NRH:qui oxidoreductase 2; NQO2; NAD(P)H qui oxidoreductase 2
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Representative Drug(s) Melatonin Drug Info Ki = 27.6 nM [4]
Co-Target Name Histamine H3 receptor (H3R) Clinical trial Target
UniProt ID HRH3_HUMAN
Gene Name HRH3
Synonyms
Histamine receptor 3; HH3R; GPCR97; G-protein coupled receptor 97; G protein-coupled receptor 97
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Representative Drug(s) Melatonin Drug Info Ki = 0.5 nM [5]
References  Top
REF 1 Synthesis, chiral resolution, absolute configuration assignment and pharmacological evaluation of a series of melatoninergic ligands. Medchemcomm. 2014;5:1303-8.
REF 2 Synthesis of a novel series of tricyclic indan derivatives as melatonin receptor agonists. J Med Chem. 2002 Sep 12;45(19):4222-39.
REF 3 Novel N-Acetyl Bioisosteres of Melatonin: Melatonergic Receptor Pharmacology, Physicochemical Studies, and Phenotypic Assessment of Their Neurogenic Potential. J Med Chem. 2015 Jun 25;58(12):4998-5014.
REF 4 Synthesis of a novel series of benzocycloalkene derivatives as melatonin receptor agonists. J Med Chem. 2002 Sep 12;45(19):4212-21.
REF 5 New Dual Small Molecules for Alzheimer's Disease Therapy Combining Histamine H 3 Receptor (H3R) Antagonism and Calcium Channels Blockade with Additional Cholinesterase Inhibition. J Med Chem. 2019 Dec 26;62(24):11416-11422.

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