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) |
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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 35:
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]
