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Ligand Lorazepam Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
Basic Ligand Information
C1 5 H1 0 ClN2 O2
Lorazepam
DIWRORZWFLOCLC-UHFFFAOYSA-N
Roles as Enzyme Ligand
Substrate in Enzyme-catalyzed Reactions (3 results)
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lorazepam + UDP-glucuronate = ?
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UDP-glucuronate + lorazepam = UDP + beta-D-glucuronosyl-lorazepam
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UDP-glucuronate + lorazepam = UDP + lorazepam beta-D-glucuronoside
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Inhibitor in Enzyme-catalyzed Reactions (1 result)
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IC50 for morphine 3-glucuronide formation: 0.065 mM (mixed type inhibition), IC50 for morphine 3-glucuronide formation: 0.056 mM (mixed type inhibition)
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Enzyme Kinetic Parameters
Ki Value (4 results)
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0.017
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Kii, morphine 6-glucuronosyltransferase activity
0.053
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Kii, morphine 3-glucuronosyltransferase activity
0.065
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Kis, morphine 6-glucuronosyltransferase activity
0.239
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Kis, morphine 3-glucuronosyltransferase activity
IC50 Value (2 results)
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0.056
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IC50 for morphine 3-glucuronide formation: 0.056 mM (mixed type inhibition)
0.065
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IC50 for morphine 3-glucuronide formation: 0.065 mM (mixed type inhibition)
References & Links Literature References (4)
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Cloning and characterisation of the first drug-metabolising canine UDP-glucuronosyltransferase of the 2B subfamily
2003
Soars, M.G.; Fettes, M.; O'Sullivan, A.C.; Riley, R.J.; Ethell, B.T.; Burchell, B.
Biochem. Pharmacol.
65
1251-1259
Morphine glucuronosyltransferase activity in human liver microsomes is inhibited by a variety of drugs that are co-administered with morphine
2007
Hara, Y.; Nakajima, M.; Miyamoto, K.; Yokoi, T.
Drug Metab. Pharmacokinet.
22
103-112
Roles of human UDP-glucuronosyltransferases in clearance and homeostasis of endogenous substrates, and functional implications
2015
Bock, K.W.
Biochem. Pharmacol.
96
77-82
Quantitative prediction of drug disposition for uridine diphosphate-glucuronosyltransferase substrates using humanized mice
2025
Miyake, T.; Fujita, Y.; Hirabayashi, M.; Komiyama, N.; Morita, K.; Tachibana, T.; Terao, K.
Drug Metab. Dispos.
53
100050
Links to other databases for Lorazepam