triazolam [Ligand Id: 7313] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL646 (Halcion, Kention, N05CD05, Triazolam, Triazolam civ, U-33,030, U-33030) |
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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 | Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreas | B | 4.41 | pIC50 | 39000 | nM | IC50 | J Med Chem (1988) 31: 176-181 [PMID:3336017] |
| CCK2 receptor/Cholecystokinin B receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL298] [GtoPdb: 77] [UniProtKB: P32239] | ||||||||
| ChEMBL | Displacement of [125I]gastrin from guinea pig gastric glands | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1988) 31: 176-181 [PMID:3336017] |
| 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 | Binding affinity to GABAA α1β2γ2 receptor. | - | 9 | pKd | 1 | nM | Kd | J Med Chem (2008) 51: 3788-803 [PMID:18537233] |
| ChEMBL | Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-1-beta-3-gamma-2 | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| GtoPdb | Binding affinity for human recombinant GABAA receptor α1β3&gamma,2. | - | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| 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] | ||||||||
| ChEMBL | Binding affinity to human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-2-beta-3-gamma-2 | B | 9.23 | pKi | 0.59 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| GtoPdb | Binding affinity to human recombinant GABAA receptor α2β3γ2. | - | 9.23 | pKi | 0.59 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| 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 | Binding affinity to human recombinant GABAA receptor α3β3γ2. | - | 8.84 | pKi | 1.43 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| ChEMBL | Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-3-beta-3-gamma-2 | B | 8.84 | pKi | 1.43 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| 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 | Binding affinity to GABAA receptor α5β2γ2. | - | 8.4 | pKd | 4 | nM | Kd | J Med Chem (2008) 51: 3788-803 [PMID:18537233] |
| GtoPdb | Binding affinity for human recombinant GABAA receptor α5β3γ2. | - | 8.81 | pKi | 1.54 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| ChEMBL | Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-5-beta-3-gamma-2 | B | 8.81 | pKi | 1.54 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| 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 | pKi | >10000 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| 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 | Binding affinity to GABAA receptor α5β2γ2. | - | 8.4 | pKd | 4 | nM | Kd | J Med Chem (2008) 51: 3788-803 [PMID:18537233] |
| GtoPdb | Binding affinity to GABAA α1β2γ2 receptor. | - | 9 | pKd | 1 | nM | Kd | J Med Chem (2008) 51: 3788-803 [PMID:18537233] |
| GtoPdb | Binding affinity for human recombinant GABAA receptor α5β3γ2. | - | 8.81 | pKi | 1.54 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| GtoPdb | Binding affinity to human recombinant GABAA receptor α3β3γ2. | - | 8.84 | pKi | 1.43 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| GtoPdb | Binding affinity for human recombinant GABAA receptor α1β3&gamma,2. | - | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| GtoPdb | Binding affinity to human recombinant GABAA receptor α2β3γ2. | - | 9.23 | pKi | 0.59 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| 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 | Binding affinity for Diazepam insensitive (DI) isoform of the benzodiazepine (Bz) binding site on GABAA receptors | B | 5.68 | pKi | 2086 | nM | Ki | J Med Chem (1993) 36: 1820-1830 [PMID:8390574] |
| ChEMBL | Binding affinity for Diazepam sensitive (DS) isoform of the benzodiazepine (Bz) binding site on GABAA receptors | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (1993) 36: 1820-1830 [PMID:8390574] |
| GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867] | ||||||||
| GtoPdb | Binding affinity to GABAA α1β2γ2 receptor. | - | 9 | pKd | 1 | nM | Kd | J Med Chem (2008) 51: 3788-803 [PMID:18537233] |
| ChEMBL | Binding affinity to GABAA alpha-1-beta-2-gamma-2 receptor | B | 9 | pKd | 1 | nM | Kd | J Med Chem (2008) 51: 3788-3803 [PMID:18537233] |
| GtoPdb | Binding affinity for human recombinant GABAA receptor α1β3&gamma,2. | - | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| 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 | 8.4 | pKd | 4 | nM | Kd | J Med Chem (2008) 51: 3788-3803 [PMID:18537233] |
| GtoPdb | Binding affinity to GABAA receptor α5β2γ2. | - | 8.4 | pKd | 4 | nM | Kd | J Med Chem (2008) 51: 3788-803 [PMID:18537233] |
| GtoPdb | Binding affinity for human recombinant GABAA receptor α5β3γ2. | - | 8.81 | pKi | 1.54 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| Platelet activating factor receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5136] [UniProtKB: P21556] | ||||||||
| ChEMBL | Inhibition of PAF-induced platelet aggregation in rabbit platelet rich plasma | F | 4.95 | pIC50 | 11100 | nM | IC50 | J Med Chem (1993) 36: 580-590 [PMID:8496938] |
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]
