Reaction Details |
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Target | Kappa-type opioid receptor |
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Ligand | BDBM50318680 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_633488 (CHEMBL1119300) |
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EC50 | 6.0±n/a nM |
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Citation | Runyon, SP; Brieaddy, LE; Mascarella, SW; Thomas, JB; Navarro, HA; Howard, JL; Pollard, GT; Carroll, FI Analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity. J Med Chem53:5290-301 (2010) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Kappa-type opioid receptor |
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Name: | Kappa-type opioid receptor |
Synonyms: | K-OR-1 | KOR-1 | Kappa-opioid receptor (KOR) | Kappa-type opioid receptor (KOPR) | Kappa-type opioid receptor (KOR) | Kappa-type opioid receptor (Kappa) | OPIATE Kappa | OPRK | OPRK1 | OPRK_HUMAN | kappa opioid receptor (KOR) |
Type: | G Protein-Coupled Receptor (GPCR) |
Mol. Mass.: | 42648.76 |
Organism: | Homo sapiens (Human) |
Description: | P41145 |
Residue: | 380 |
Sequence: | MDSPIQIFRGEPGPTCAPSACLPPNSSAWFPGWAEPDSNGSAGSEDAQLEPAHISPAIPV
IITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSTVYL
MNSWPFGDVLCKIVISIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINI
CIWLLSSSVGISAIVLGGTKVREDVDVIECSLQFPDDDYSWWDLFMKICVFIFAFVIPVL
IIIVCYTLMILRLKSVRLLSGSREKDRNLRRITRLVLVVVAVFVVCWTPIHIFILVEALG
STSHSTAALSSYYFCIALGYTNSSLNPILYAFLDENFKRCFRDFCFPLKMRMERQSTSRV
RNTVQDPAYLRDIDGMNKPV
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BDBM50318680 |
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n/a |
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Name | BDBM50318680 |
Synonyms: | 7-HYDROXY-2-OXO-2-ISOTHIOCHROMAN-3(+)-CARBOXYLIC ACID-{1-[4-(3-HYDROXYPHENYL)-(3R,4R)-TRANS-DIMETHYL-PIPERIDINYLMETHYL]-(2S)-METHYLPROPYL}AMIDE (DIASTEREOMERIC MIX) | 7-Hydroxy-2-oxo-2-isothiochroman-3(+)-carboxylic acid-{1-[4-(3-hydroxyphenyl)-(3R,4R)-trans-dimethyl-piperidinylmethyl]-(2S)-methylpropyl}amide | CHEMBL1083372 |
Type | Small organic molecule |
Emp. Form. | C28H38N2O4S |
Mol. Mass. | 498.677 |
SMILES | CC(C)[C@@H](CN1CC[C@](C)([C@@H](C)C1)c1cccc(O)c1)NC(=O)[C@H]1Cc2ccc(O)cc2CS1=O |r| |
Structure |
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