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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL13280 (Flunitrazepam, N05CD03, RO 5-4200, RO-54200, RO-5-4200, Rohypnol)
  • CCK1 receptor/Cholecystokinin A receptor in Rat [ChEMBL: CHEMBL2871] [GtoPdb: 76] [UniProtKB: P30551]
  • Cholecystokinin A receptor in Guinea pig [ChEMBL: CHEMBL3501] [UniProtKB: Q63931]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867]
There should be some charts here, you may need to enable JavaScript!
  • GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Human [ChEMBL: CHEMBL5112] [GtoPdb: 408] [UniProtKB: P31644]
There should be some charts here, you may need to enable JavaScript!
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 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 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 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]

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]