flunitrazepam [Ligand Id: 4193] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL13280 (Flunitrazepam, N05CD03, RO 5-4200, RO-5-4200, RO-54200, Rohypnol)
  • CCK1 receptor/Cholecystokinin A receptor in Rat [ChEMBL: CHEMBL2871] [GtoPdb: 76] [UniProtKB: P30551]
  • Cholecystokinin A receptor in Guinea pig [ChEMBL: CHEMBL3501] [UniProtKB: Q63931]
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  • GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2095172] [GtoPdb: 404, 414, 411] [UniProtKB: P14867, P18507, P47870]
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  • GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABA-A receptor; alpha-1/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094121] [GtoPdb: 404, 414, 412] [UniProtKB: P14867, P18507, P28472]
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  • GABAA receptor γ2 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-2/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2111413] [GtoPdb: 414, 405, 411] [UniProtKB: P18507, P47869, P47870]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α2 subunit/GABA-A receptor; alpha-2/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094130] [GtoPdb: 414, 412, 405] [UniProtKB: P18507, P28472, P47869]
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  • GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2111339] [GtoPdb: 414, 406, 411] [UniProtKB: P18507, P34903, P47870]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α3 subunit/GABA-A receptor; alpha-3/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094120] [GtoPdb: 414, 412, 406] [UniProtKB: P18507, P28472, P34903]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABA-A receptor; alpha-5/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094122] [GtoPdb: 414, 412, 408] [UniProtKB: P18507, P28472, P31644]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α6 subunit/GABA-A receptor; alpha-6/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2095190] [GtoPdb: 414, 412, 409] [UniProtKB: P18507, P28472, Q16445]
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  • GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867]
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  • GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Human [ChEMBL: CHEMBL5112] [GtoPdb: 408] [UniProtKB: P31644]
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  • GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor β2 subunit/Gamma-aminobutyric acid receptor subunit alpha-5/beta-2/gamma-2 in Human [ChEMBL: CHEMBL4523641] [GtoPdb: 414, 408, 411] [UniProtKB: P18507, P31644, P47870]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CCK1 receptor/Cholecystokinin A receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2871] [GtoPdb: 76] [UniProtKB: P30551]
ChEMBL Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue B 4 pIC50 >100000 nM IC50 J Med Chem (1988) 31: 2235-2246 [PMID:2848124]
Cholecystokinin A receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3501] [UniProtKB: Q63931]
ChEMBL Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor B 4 pIC50 >100000 nM IC50 J Med Chem (1987) 30: 1229-1239 [PMID:2885419]
GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095172] [GtoPdb: 404, 414, 411] [UniProtKB: P14867, P18507, P47870]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α1β3γ2. - 8.28 pKi 5.2 nM Ki Mol Pharmacol (1996) 49: 253-9 [PMID:8632757]
ChEMBL Binding affinity evaluated by ability to displace [3H]Ro-151788 from recombinant human Gamma-aminobutyric acid A receptor alpha-1-beta-2-gamma-2 expressed in L(tk-)cells B 8.41 pKi 3.9 nM Ki Bioorg Med Chem Lett (2000) 10: 1381-1384 [PMID:10890169]
ChEMBL Displacement of [3H]flunitrazepam from human recombinant alpha1beta2gamma2 GABAA receptor expressed in HEK cell membrane by competitive radioligand binding assay B 8.66 pKi 2.2 nM Ki Bioorg Med Chem Lett (2022) 62: 128637-128637 [PMID:35218882]
ChEMBL Activity at human GABAA alpha-1-beta-2-gamma-2 LS327A,S343A receptor in HEK293 cells expressing as-PKCepsilon assessed as evoked current response by whole cell patch clamp method B 1.46 pEC50 1.46 - logEC50 J Biol Chem (2007) 282: 33052-33063 [PMID:17875639]
ChEMBL Activity at human GABAA alpha-1-beta-2-gamma-2 LS327A receptor in HEK293 cells expressing as-PKCepsilon assessed as evoked current response by whole cell patch clamp method B 1.46 pEC50 1.46 - logEC50 J Biol Chem (2007) 282: 33052-33063 [PMID:17875639]
ChEMBL Activity at human GABAA alpha-1-beta-2-gamma-2S327 receptor in HEK293 cells expressing as-PKCepsilon cells assessed as evoked current response by whole cell patch clamp method B 8.85 pEC50 1.4 nM EC50 J Biol Chem (2007) 282: 33052-33063 [PMID:17875639]
GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABA-A receptor; alpha-1/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094121] [GtoPdb: 404, 414, 412] [UniProtKB: P14867, P18507, P28472]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α1β3γ2. - 8.28 pKi 5.2 nM Ki Mol Pharmacol (1996) 49: 253-9 [PMID:8632757]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-1-beta-3-gamma-2 B 8.66 pKi 2.2 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
ChEMBL Binding affinity measured using LtK- cell membranes expressing GABA alpha-1-beta-3-gamma-2 receptor B 8.66 pKi 2.2 nM Ki J Med Chem (1998) 41: 2537-2552 [PMID:9651158]
GABAA receptor γ2 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-2/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111413] [GtoPdb: 414, 405, 411] [UniProtKB: P18507, P47869, P47870]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α2β1γ2. - 8.28 pKi 5.2 nM Ki Mol Pharmacol (1996) 49: 253-9 [PMID:8632757]
ChEMBL Displacement of [3H]flunitrazepam from human recombinant alpha2beta2gamma2 GABAA receptor expressed in HEK cell membrane by competitive radioligand binding assay B 8.6 pKi 2.5 nM Ki Bioorg Med Chem Lett (2022) 62: 128637-128637 [PMID:35218882]
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α2 subunit/GABA-A receptor; alpha-2/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094130] [GtoPdb: 414, 412, 405] [UniProtKB: P18507, P28472, P47869]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α2β1γ2. - 8.28 pKi 5.2 nM Ki Mol Pharmacol (1996) 49: 253-9 [PMID:8632757]
ChEMBL Binding affinity to human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-2-beta-3-gamma-2 B 8.6 pKi 2.5 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
ChEMBL Binding affinity measured using LtK- cell membranes expressing GABA alpha-2-beta-3-gamma-2 receptor B 8.6 pKi 2.5 nM Ki J Med Chem (1998) 41: 2537-2552 [PMID:9651158]
ChEMBL Binding affinity evaluated by ability to displace [3H]-Ro-15-1788 from recombinant human Gamma-aminobutyric acid A receptor alpha-2-beta-3-gamma-2 expressed in L(tk-)cells B 8.96 pKi 1.1 nM Ki Bioorg Med Chem Lett (2000) 10: 1381-1384 [PMID:10890169]
GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111339] [GtoPdb: 414, 406, 411] [UniProtKB: P18507, P34903, P47870]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α3β1γ2. - 7.8 pKi 15.7 nM Ki Mol Pharmacol (1996) 49: 253-9 [PMID:8632757]
ChEMBL Displacement of [3H]flunitrazepam from human recombinant alpha3beta2gamma2 GABAA receptor expressed in HEK cell membrane by competitive radioligand binding assay B 8.35 pKi 4.5 nM Ki Bioorg Med Chem Lett (2022) 62: 128637-128637 [PMID:35218882]
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α3 subunit/GABA-A receptor; alpha-3/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094120] [GtoPdb: 414, 412, 406] [UniProtKB: P18507, P28472, P34903]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α3β1γ2. - 7.8 pKi 15.7 nM Ki Mol Pharmacol (1996) 49: 253-9 [PMID:8632757]
ChEMBL Binding affinity evaluated by ability to displace [3H]Ro-151788 from recombinant human Gamma-aminobutyric acid A receptor alpha-3-beta-3-gamma-2 expressed in L(tk-)cells B 8.23 pKi 5.9 nM Ki Bioorg Med Chem Lett (2000) 10: 1381-1384 [PMID:10890169]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-3-beta-3-gamma-2 B 8.35 pKi 4.5 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
ChEMBL Binding affinity measured using LtK- cell membranes expressing GABA alpha-3-beta-3-gamma-2 receptor B 8.35 pKi 4.5 nM Ki J Med Chem (1998) 41: 2537-2552 [PMID:9651158]
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABA-A receptor; alpha-5/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094122] [GtoPdb: 414, 412, 408] [UniProtKB: P18507, P28472, P31644]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α5β1γ2. - 8.26 pKi 5.5 nM Ki Mol Pharmacol (1996) 49: 253-9 [PMID:8632757]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-5-beta-3-gamma-2 B 8.68 pKi 2.1 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
ChEMBL Binding affinity measured using LtK- cell membranes expressing Gamma-aminobutyric acid A receptor alpha-5-beta-3-gamma-2 B 8.68 pKi 2.1 nM Ki J Med Chem (1998) 41: 2537-2552 [PMID:9651158]
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α6 subunit/GABA-A receptor; alpha-6/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095190] [GtoPdb: 414, 412, 409] [UniProtKB: P18507, P28472, Q16445]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-6-beta-3-gamma-2 B 5.7 pKi >2000 nM Ki J Med Chem (2000) 43: 71-95 [PMID:10633039]
ChEMBL Binding affinity measured using LtK- cell membranes expressing Gamma-aminobutyric acid A receptor alpha-6-beta-3-gamma-2 B 5.7 pKi >2000 nM Ki J Med Chem (1998) 41: 2537-2552 [PMID:9651158]
GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit in Human [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O00591, P18505, O14764, P18507, P31644, P34903, Q8N1C3, P47869, P48169, Q99928, Q16445, P14867, P28472, P47870, P78334]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α3β1γ2. - 7.8 pKi 15.7 nM Ki Mol Pharmacol (1996) 49: 253-9 [PMID:8632757]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α5β1γ2. - 8.26 pKi 5.5 nM Ki Mol Pharmacol (1996) 49: 253-9 [PMID:8632757]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α1β3γ2. - 8.28 pKi 5.2 nM Ki Mol Pharmacol (1996) 49: 253-9 [PMID:8632757]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α2β1γ2. - 8.28 pKi 5.2 nM Ki Mol Pharmacol (1996) 49: 253-9 [PMID:8632757]
GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit/GABA-A receptor; anion channel in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907607] [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O09028, P15431, P18506, P18508, P19969, P20236, P23574, P23576, P28471, P28473, P30191, P62813, P63079, P63138, Q91ZM7, Q9ES14]
ChEMBL Displacement of [3H]beta-CCE from GABA-A benzodiazepine receptor of rat cerebral cortex membranes B 8.1 pIC50 8 nM IC50 J Med Chem (1987) 30: 1248-1254 [PMID:3037081]
ChEMBL Displacement of [3H]flunitrazepam from GABA-A benzodiazepine receptor of rat cerebral cortex membrane B 8.52 pIC50 3 nM IC50 J Med Chem (1987) 30: 1248-1254 [PMID:3037081]
ChEMBL Inhibition of [3H]diazepam binding to GABA-A benzodiazepine receptor of rat brain B 8.77 pIC50 1.7 nM IC50 J Med Chem (1988) 31: 2235-2246 [PMID:2848124]
ChEMBL Displacement of [3H]diazepam from rat brain GABA-A benzodiazepine receptor B 8.77 pIC50 1.7 nM IC50 J Med Chem (1987) 30: 1229-1239 [PMID:2885419]
ChEMBL Displacement of [3H]diazepam from GABA-A Benzodiazepine receptor of rat forebrain B 8.82 pIC50 1.5 nM IC50 J Med Chem (1991) 34: 281-290 [PMID:1846920]
GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867]
ChEMBL Binding affinity to GABAA alpha-1-beta-2-gamma-2 receptor B 8.35 pKd 4.5 nM Kd J Med Chem (2008) 51: 3788-3803 [PMID:18537233]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α1β3γ2. - 8.28 pKi 5.2 nM Ki Mol Pharmacol (1996) 49: 253-9 [PMID:8632757]
ChEMBL Activity at human GABAA alpha-1-beta-2-gamma-2L receptor in HEK293 cells expressing as-PKCepsilon assessed as evoked current response by whole cell patch clamp method B 1.99 pEC50 1.99 - logEC50 J Biol Chem (2007) 282: 33052-33063 [PMID:17875639]
GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5112] [GtoPdb: 408] [UniProtKB: P31644]
ChEMBL Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptor B 8.52 pKd 3 nM Kd J Med Chem (2008) 51: 3788-3803 [PMID:18537233]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α5β1γ2. - 8.26 pKi 5.5 nM Ki Mol Pharmacol (1996) 49: 253-9 [PMID:8632757]
GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor β2 subunit/Gamma-aminobutyric acid receptor subunit alpha-5/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4523641] [GtoPdb: 414, 408, 411] [UniProtKB: P18507, P31644, P47870]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α5β1γ2. - 8.26 pKi 5.5 nM Ki Mol Pharmacol (1996) 49: 253-9 [PMID:8632757]
ChEMBL Displacement of [3H]flunitrazepam from human recombinant alpha5beta2gamma2 GABAA receptor expressed in HEK cell membrane by competitive radioligand binding assay B 8.68 pKi 2.1 nM Ki Bioorg Med Chem Lett (2022) 62: 128637-128637 [PMID:35218882]

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]