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/GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2095172] [GtoPdb: 404, 414, 411] [UniProtKB: P14867, P18507, P47870]
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  • GABAA receptor γ2 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-2/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2111413] [GtoPdb: 414, 405, 411] [UniProtKB: P18507, P47869, P47870]
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  • GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2111339] [GtoPdb: 414, 406, 411] [UniProtKB: P18507, P34903, P47870]
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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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  • GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor β2 subunit/Gamma-aminobutyric acid receptor subunit alpha-5/beta-2/gamma-2 in Human [ChEMBL: CHEMBL4523641] [GtoPdb: 414, 408, 411] [UniProtKB: P18507, P31644, P47870]
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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 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]
ChEMBL Displacement of [3H]flunitrazepam from human recombinant alpha1beta2gamma2 GABAA receptor expressed in HEK cell membrane by competitive radioligand binding assay B 9.1 pKi 0.8 nM Ki Bioorg Med Chem Lett (2022) 62: 128637-128637 [PMID:35218882]
GtoPdb - - 7.43 pEC50 37 nM EC50 J Med Chem (2002) 45: 5043-51 [PMID:12408715]
GABAA receptor γ2 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-2/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111413] [GtoPdb: 414, 405, 411] [UniProtKB: P18507, P47869, P47870]
ChEMBL Displacement of [3H]flunitrazepam from human recombinant alpha2beta2gamma2 GABAA receptor expressed in HEK cell membrane by competitive radioligand binding assay B 9.22 pKi 0.6 nM Ki Bioorg Med Chem Lett (2022) 62: 128637-128637 [PMID:35218882]
GtoPdb - - 7.92 pEC50 12 nM EC50 J Med Chem (2002) 45: 5043-51 [PMID:12408715]
GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111339] [GtoPdb: 414, 406, 411] [UniProtKB: P18507, P34903, P47870]
ChEMBL Displacement of [3H]flunitrazepam from human recombinant alpha3beta2gamma2 GABAA receptor expressed in HEK cell membrane by competitive radioligand binding assay B 8.85 pKi 1.4 nM Ki Bioorg Med Chem Lett (2022) 62: 128637-128637 [PMID:35218882]
GtoPdb - - 7.16 pEC50 69 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 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]
GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor β2 subunit/Gamma-aminobutyric acid receptor subunit alpha-5/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4523641] [GtoPdb: 414, 408, 411] [UniProtKB: P18507, P31644, P47870]
ChEMBL Displacement of [3H]flunitrazepam from human recombinant alpha5beta2gamma2 GABAA receptor expressed in HEK cell membrane by competitive radioligand binding assay B 8.82 pKi 1.5 nM Ki Bioorg Med Chem Lett (2022) 62: 128637-128637 [PMID:35218882]
GtoPdb - - 8 pEC50 10 nM EC50 J Med Chem (2002) 45: 5043-51 [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 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]