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 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]
