alprazolam [Ligand Id: 7111] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL661 (Alprazolam, Alprazolam civ, Niravam, NSC-760140, U 31,889, U-31,889, U-31889, Xanax, Xanax xr)
  • bromodomain containing 4/Bromodomain-containing protein 4 in Human [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
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  • CCK1 receptor/Cholecystokinin A receptor in Rat [ChEMBL: CHEMBL2871] [GtoPdb: 76] [UniProtKB: P30551]
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  • CCK2 receptor/Cholecystokinin B receptor in Human [ChEMBL: CHEMBL298] [GtoPdb: 77] [UniProtKB: P32239]
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  • GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867]
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  • GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Human [ChEMBL: CHEMBL4956] [GtoPdb: 405] [UniProtKB: P47869]
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  • GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Human [ChEMBL: CHEMBL3026] [GtoPdb: 406] [UniProtKB: P34903]
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  • GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Human [ChEMBL: CHEMBL5112] [GtoPdb: 408] [UniProtKB: P31644]
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  • Platelet activating factor receptor in Guinea pig [ChEMBL: CHEMBL5136] [UniProtKB: P21556]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
ChEMBL Binding affinity to BRD4-BD1 by isothermal titration calorimetry B 5.61 pKd 2460 nM Kd Bioorg Med Chem (2012) 20: 1878-1886 [PMID:22137933]
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 4.19 pIC50 64000 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 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 - - 7.16 pEC50 69 nM EC50 J Med Chem (2002) 45: 5043-51 [PMID:12408715]
GtoPdb - - 7.43 pEC50 37 nM EC50 J Med Chem (2002) 45: 5043-51 [PMID:12408715]
GtoPdb - - 7.92 pEC50 12 nM EC50 J Med Chem (2002) 45: 5043-51 [PMID:12408715]
GtoPdb - - 8 pEC50 10 nM EC50 J Med Chem (2002) 45: 5043-51 [PMID:12408715]
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 was determined by displacement of [3H]flumazenil from rat cortex homogenates F 8.48 pKi 3.3 nM Ki J Med Chem (2002) 45: 5043-5051 [PMID:12408715]
GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867]
GtoPdb - - 7.43 pEC50 37 nM EC50 J Med Chem (2002) 45: 5043-51 [PMID:12408715]
ChEMBL Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 1 B 7.43 pEC50 37 nM EC50 J Med Chem (2002) 45: 5043-5051 [PMID:12408715]
GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4956] [GtoPdb: 405] [UniProtKB: P47869]
GtoPdb - - 7.92 pEC50 12 nM EC50 J Med Chem (2002) 45: 5043-51 [PMID:12408715]
ChEMBL Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 2 B 7.92 pEC50 12 nM EC50 J Med Chem (2002) 45: 5043-5051 [PMID:12408715]
GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3026] [GtoPdb: 406] [UniProtKB: P34903]
GtoPdb - - 7.16 pEC50 69 nM EC50 J Med Chem (2002) 45: 5043-51 [PMID:12408715]
ChEMBL Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 3 B 7.16 pEC50 69 nM EC50 J Med Chem (2002) 45: 5043-5051 [PMID:12408715]
GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5112] [GtoPdb: 408] [UniProtKB: P31644]
GtoPdb - - 8 pEC50 10 nM EC50 J Med Chem (2002) 45: 5043-51 [PMID:12408715]
ChEMBL Effective concentration against Gamma-aminobutyric acid A receptor, alpha 5 B 8 pEC50 10 nM EC50 J Med Chem (2002) 45: 5043-5051 [PMID:12408715]
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 4.66 pIC50 22000 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]