triazolam [Ligand Id: 7313] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL646 (Halcion, N05CD05, Triazolam, U-33030, U-33,030, Kention, Triazolam civ)
  • CCK1 receptor/Cholecystokinin A receptor in Rat [ChEMBL: CHEMBL2871] [GtoPdb: 76] [UniProtKB: P30551]
  • This target only has 0 pki data point
  • 0
1 CHEMBL646_lig_chart_1 Cholecystokinin A receptor Rat
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  • CCK2 receptor/Cholecystokinin B receptor in Human [ChEMBL: CHEMBL298] [GtoPdb: 77] [UniProtKB: P32239]
  • This target only has 0 pki data point
  • 0
2 CHEMBL646_lig_chart_2 Cholecystokinin B receptor Human
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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: 404414412] [UniProtKB: P14867P18507P28472]
  • 9.1
3 CHEMBL646_lig_chart_3 GABA-A receptor; alpha-1/beta-3/gamma-2 Human
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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: 414412405] [UniProtKB: P18507P28472P47869]
  • 9.23
4 CHEMBL646_lig_chart_4 GABA-A receptor; alpha-2/beta-3/gamma-2 Human
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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: 414412406] [UniProtKB: P18507P28472P34903]
  • 8.84
5 CHEMBL646_lig_chart_5 GABA-A receptor; alpha-3/beta-3/gamma-2 Human
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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: 414412408] [UniProtKB: P18507P28472P31644]
  • 8.81
6 CHEMBL646_lig_chart_6 GABA-A receptor; alpha-5/beta-3/gamma-2 Human
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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: 414412409] [UniProtKB: P18507P28472Q16445]
  • This target only has 1 pki data point
  • 5
7 CHEMBL646_lig_chart_7 GABA-A receptor; alpha-6/beta-3/gamma-2 Human
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8 CHEMBL646_lig_chart_8 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 HumanRat
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  • GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867]
  • This target only has 1 pki data point
  • 9.1
9 CHEMBL646_lig_chart_9 GABA receptor alpha-1 subunit Human
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  • GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Human [ChEMBL: CHEMBL5112] [GtoPdb: 408] [UniProtKB: P31644]
  • This target only has 1 pki data point
  • 8.81
10 CHEMBL646_lig_chart_10 GABA receptor alpha-5 subunit Human
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  • Platelet activating factor receptor in Guinea pig [ChEMBL: CHEMBL5136] [UniProtKB: P21556]
  • This target only has 0 pki data point
  • 0
11 CHEMBL646_lig_chart_11 Platelet activating factor receptor Guinea pig
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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: 404414412] [UniProtKB: P14867P18507P28472]
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: 414412405] [UniProtKB: P18507P28472P47869]
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: 414412406] [UniProtKB: P18507P28472P34903]
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: 414412408] [UniProtKB: P18507P28472P31644]
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: 414412409] [UniProtKB: P18507P28472Q16445]
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: 419410416414408406413405407415409404412411417] [UniProtKB: O00591P18505O14764P18507P31644P34903Q8N1C3P47869P48169Q99928Q16445P14867P28472P47870P78334]
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: 419410416414408406413405407415409404412411417] [UniProtKB: O09028P15431P18506P18508P19969P20236P23574P23576P28471P28473P30191P62813P63079P63138Q91ZM7Q9ES14]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]