Details of the Biological Target of DIG (DBT)
General Information of DBT (ID: ET03SPZ) | |||||
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Name |
Opioid receptor kappa (OPRK1)
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Synonyms |
Click to Show/Hide the Synonyms of This DBT
Kappa opioid receptor; Kappa-type opioid receptor; K-OR-1; KOR; KOR-1; OPRK
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Family | G-protein coupled receptor (GPCR) >> G-protein coupled rhodopsin receptor (GPCR-A) | ||||
Organism |
Homo sapiens (Human)
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Gene Name | OPRK1 | Gene ID | |||
UniProt ID | OPRK_HUMAN | (click to find more protein-related data of this DBT) | |||
TTD ID | T60693 | (click to find more therapeutic target data of this DBT) | |||
Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target | |||||
Sequence |
MDSPIQIFRGEPGPTCAPSACLPPNSSAWFPGWAEPDSNGSAGSEDAQLEPAHISPAIPV
IITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSTVYL MNSWPFGDVLCKIVISIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINI CIWLLSSSVGISAIVLGGTKVREDVDVIECSLQFPDDDYSWWDLFMKICVFIFAFVIPVL IIIVCYTLMILRLKSVRLLSGSREKDRNLRRITRLVLVVVAVFVVCWTPIHIFILVEALG STSHSTAALSSYYFCIALGYTNSSLNPILYAFLDENFKRCFRDFCFPLKMRMERQSTSRV RNTVQDPAYLRDIDGMNKPV |
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Function |
Functions as receptor for various synthetic opioids and for the psychoactive diterpene salvinorin A. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance.
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Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT | ||||||
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DIG Name: Simethicone | Click to Show/Hide | |||||
Detailed Information |
DIG Info
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Functional Class | Click to Show/Hide the Functional Class of This DIG
Antifoaming agent; Diluent; Water-repelling agent
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Experiment for Assessing the Biological Activity of This DIG on the Studied DBT | ||||||
Biological Activity | IC50 = 155 nM (estimated based on the structural similarity with CHEMBL1707 ) | [1] | ||||
Structural Similarity | Tanimoto coefficient = 0.942028986 | |||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | OPRK_HUMAN | |||||
References | |||||
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1 | From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands. J Med Chem. 2001 Oct 11; 44(21):3378-90. | ||||
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