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-5-4200, RO-54200, Rohypnol) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 33:
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]
