diazepam [Ligand Id: 3364] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL12 (Alupram 10, Alupram 2, Alupram 5, Ansiolisina, Apozepam, Atensine, Centrazepam, Diacepin, Dialar, Dialar fte, Diastat, Diastat acudial, Diazepam, Diazepam civ, Diazepam intensol, Dizac, E-Pam, LA III, LA-III, Nrl-1, NRL-1, NSC-169897, NSC-77518, Paxel, Q-pam, Relanium, RO 5-2807, RO-5-2807, RO-52807, Scriptopam, Serenack, Servizepam, Solis, Stesolid, Tensium, Tranimul, Tranquase, Valclair, Valium, Valrelease, Valtoco, Vivol, WY-3467) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Acetylcholinesterase in Electrophorus electricus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4078] [UniProtKB: O42275] | ||||||||
| ChEMBL | Inhibition of Electrophorus electricus (electric eel) acetylcholinesterase (AChE) assessed as inhibition of ATCh hydrolysis by Ellman method | B | 4.89 | pKi | 13000 | nM | Ki | Med Chem Res (2005) 14: 297-308 |
| Aldo-keto reductase family 1 member C1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5905] [UniProtKB: Q04828] | ||||||||
| ChEMBL | Discontinuous Radiometric Assay: Compounds may be evaluated as selective reversible inhibitors of AKR1C3 by screening them against homogeneous recombinant AKR1C1-AKR1C4 expressed in E. coli. In each case, a discontinuous radiometric assay may be used to monitor the inhibition of progesterone reduction (20-ketosteroid reduction) catalyzed by AKR1C1, the inhibition of Δ4-AD reduction (17-ketosteroid reduction) catalyzed by AKR1C3, and the inhibition of 5α-DHT reduction (3-ketosteroid reduction) catalyzed by AKR1C2 and AKR1C4 (by measuring the formation of 20α-hydroxyprogesterone, testosterone or 3α-androstanediol by radiochromatography). Secondary screens of the compounds of interest include: (a) a full-screen against all nine human recombinant AKR enzymes to ensure there are no-intended off-target effects (in this context AKR1B10 (retinal reductase; SEQ ID NO:5) has been shown to be potently inhibited by N-phenylanthranilates) (Endo et al., 2010, Biol. Pharm. Bull. 33:886-90); (b) a screen against COX-1 and COX-2 to reaffirm that compounds do not act as NSAIDs; and (c) an expanded screen against other nuclear receptors (especially other steroid hormone receptors). | B | 5.25 | pIC50 | 5600 | nM | IC50 | US-9271961-B2. Bifunctional AKR1C3 inhibitors/androgen receptor modulators and methods of use thereof (2016) |
| Aldo-keto reductase family 1 member C2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5847] [UniProtKB: P52895] | ||||||||
| ChEMBL | Discontinuous Radiometric Assay: Compounds may be evaluated as selective reversible inhibitors of AKR1C3 by screening them against homogeneous recombinant AKR1C1-AKR1C4 expressed in E. coli. In each case, a discontinuous radiometric assay may be used to monitor the inhibition of progesterone reduction (20-ketosteroid reduction) catalyzed by AKR1C1, the inhibition of Δ4-AD reduction (17-ketosteroid reduction) catalyzed by AKR1C3, and the inhibition of 5α-DHT reduction (3-ketosteroid reduction) catalyzed by AKR1C2 and AKR1C4 (by measuring the formation of 20α-hydroxyprogesterone, testosterone or 3α-androstanediol by radiochromatography). Secondary screens of the compounds of interest include: (a) a full-screen against all nine human recombinant AKR enzymes to ensure there are no-intended off-target effects (in this context AKR1B10 (retinal reductase; SEQ ID NO:5) has been shown to be potently inhibited by N-phenylanthranilates) (Endo et al., 2010, Biol. Pharm. Bull. 33:886-90); (b) a screen against COX-1 and COX-2 to reaffirm that compounds do not act as NSAIDs; and (c) an expanded screen against other nuclear receptors (especially other steroid hormone receptors). | B | 5.62 | pIC50 | 2400 | nM | IC50 | US-9271961-B2. Bifunctional AKR1C3 inhibitors/androgen receptor modulators and methods of use thereof (2016) |
| AKR1C3/Aldo-keto-reductase family 1 member C3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4681] [GtoPdb: 1382] [UniProtKB: P42330] | ||||||||
| ChEMBL | Discontinuous Radiometric Assay: Compounds may be evaluated as selective reversible inhibitors of AKR1C3 by screening them against homogeneous recombinant AKR1C1-AKR1C4 expressed in E. coli. In each case, a discontinuous radiometric assay may be used to monitor the inhibition of progesterone reduction (20-ketosteroid reduction) catalyzed by AKR1C1, the inhibition of Δ4-AD reduction (17-ketosteroid reduction) catalyzed by AKR1C3, and the inhibition of 5α-DHT reduction (3-ketosteroid reduction) catalyzed by AKR1C2 and AKR1C4 (by measuring the formation of 20α-hydroxyprogesterone, testosterone or 3α-androstanediol by radiochromatography). Secondary screens of the compounds of interest include: (a) a full-screen against all nine human recombinant AKR enzymes to ensure there are no-intended off-target effects (in this context AKR1B10 (retinal reductase; SEQ ID NO:5) has been shown to be potently inhibited by N-phenylanthranilates) (Endo et al., 2010, Biol. Pharm. Bull. 33:886-90); (b) a screen against COX-1 and COX-2 to reaffirm that compounds do not act as NSAIDs; and (c) an expanded screen against other nuclear receptors (especially other steroid hormone receptors). | B | 4.08 | pIC50 | 84000 | nM | IC50 | US-9271961-B2. Bifunctional AKR1C3 inhibitors/androgen receptor modulators and methods of use thereof (2016) |
| CCK1 receptor/Cholecystokinin A receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2871] [GtoPdb: 76] [UniProtKB: P30551] | ||||||||
| ChEMBL | Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1988) 31: 2235-2246 [PMID:2848124] |
| Cholecystokinin A receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3501] [UniProtKB: Q63931] | ||||||||
| ChEMBL | Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1987) 30: 1229-1239 [PMID:2885419] |
| Cholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5763] [UniProtKB: P81908] | ||||||||
| ChEMBL | Inhibition of Equus caballus (horse) serum butyrylcholinesterase (BChE) assessed as inhibition of BTCh hydrolysis by Ellman method | B | 5.3 | pKi | 5011.87 | nM | Ki | Med Chem Res (2005) 14: 297-308 |
| ChEMBL | Inhibition of Equus caballus (horse) serum butyrylcholinesterase (BChE) assessed as inhibition of BTCh hydrolysis by Ellman method | B | 7.37 | pKi | 43 | nM | Ki | Med Chem Res (2005) 14: 297-308 |
| fatty acid binding protein 1/Fatty acid-binding protein, liver in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5738] [GtoPdb: 2531] [UniProtKB: P02692] | ||||||||
| ChEMBL | Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP high binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay | B | 6.27 | pKi | 531 | nM | Ki | J Med Chem (2008) 51: 3755-3764 [PMID:18533710] |
| GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 subunit/GABA A receptor alpha-1/beta-1/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111392] [GtoPdb: 404, 410, 414] [UniProtKB: P14867, P18505, P18507] | ||||||||
| GtoPdb | Assay using recombinant GABAA channels with subunit composition; α1β1γ2. | - | 7.79 | pKi | 16.3 | nM | Ki | Science (1989) 245: 1389-92 [PMID:2551039] |
| ChEMBL | Displacement of [3H]Flumazenil from human GABA-Aalpha1 receptor plus beta-2-gamma-2 expressed in HEK293 cells | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2006) 49: 2526-2533 [PMID:16610795] |
| 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] | ||||||||
| GtoPdb | Assay using recombinant GABAA channels with subunit composition; α1β1γ2. | - | 7.79 | pKi | 16.3 | nM | Ki | Science (1989) 245: 1389-92 [PMID:2551039] |
| ChEMBL | Displacement of [3H]flunitrazepam from human recombinant alpha1beta2gamma2 GABAA receptor expressed in HEK cell membrane by competitive radioligand binding assay | B | 7.85 | pKi | 14 | nM | Ki | Bioorg Med Chem Lett (2022) 62: 128637-128637 [PMID:35218882] |
| ChEMBL | Displacement of [3H]Flunitrazepam from GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in Sf9 cells | B | 7.89 | pKi | 13 | nM | Ki | J Med Chem (1996) 39: 158-175 [PMID:8568803] |
| ChEMBL | Binding affinity evaluated by ability to displace [3H]Ro-151788 from recombinant human Gamma-aminobutyric acid A receptor alpha-1-beta-2-gamma-2 expressed in L(tk-)cells | B | 7.92 | pKi | 12 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1381-1384 [PMID:10890169] |
| ChEMBL | Allosteric modulation of GABAA alpha1beta2gamma2 (unknown origin) expressed in Xenopus oocytes assessed as potentiation of GABA-induced current response at -80 mV holding potential incubated for 3 mins by two electrode voltage clamp method | B | 7 | pEC50 | 100 | nM | EC50 | Bioorg Med Chem (2016) 24: 681-685 [PMID:26791864] |
| ChEMBL | Binding affinity to human alpha1beta2gamma2 GABA receptor expressed in Xenopus laevis oocytes | B | 7.07 | pEC50 | 85 | nM | EC50 | Bioorg Med Chem (2010) 18: 8374-8382 [PMID:20980155] |
| GABAA receptor γ2 subunit/GABAA receptor α1 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095167] [GtoPdb: 414, 404, 411] [UniProtKB: P18508, P62813, P63138] | ||||||||
| ChEMBL | Binding affinity for mutant rat GABA-A receptor alpha-1-(arg)-beta-2-gamma-2 subunits expressed in HEK293 cells | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1994) 37: 4576-4580 [PMID:7799410] |
| ChEMBL | Binding affinity for rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (1994) 37: 4576-4580 [PMID:7799410] |
| ChEMBL | Displacement of [3H]Ro-151788 from rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2002) 45: 5710-5720 [PMID:12477354] |
| ChEMBL | Binding affinity for recombinant rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2003) 46: 310-313 [PMID:12519068] |
| ChEMBL | Displacement of [3H]Ro15-1788 from rat recombinant GABA alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells | B | 7.92 | pKi | 12 | nM | Ki | Bioorg Med Chem (2007) 15: 2573-2586 [PMID:17306981] |
| ChEMBL | Displacement of [3H]flumazenil from rat GABA-A alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (2009) 52: 3723-3734 [PMID:19469479] |
| ChEMBL | Displacement of [3H]Ro-151788 from rat recombinant GABA alpha-5-beta-2-gamma-2 receptor expressed in HEK293 cells | B | 8.01 | pKi | 9.8 | nM | Ki | Bioorg Med Chem (2007) 15: 2573-2586 [PMID:17306981] |
| 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 | Assay using recombinant GABAA channels with subunit composition; α1β1γ2. | - | 7.79 | pKi | 16.3 | nM | Ki | Science (1989) 245: 1389-92 [PMID:2551039] |
| ChEMBL | Binding affinity towards human alpha-1-beta-3-gamma-2 GABA-A receptor using [3H]Ro-151788 expressed in L(tk-) cells | B | 7.84 | pKi | 14.3 | nM | Ki | J Med Chem (2004) 47: 3642-3657 [PMID:15214791] |
| ChEMBL | Binding affinity for human GABA-A receptor alpha-4-beta-3-gamma-2 subunits in L(tk-) cells | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2004) 47: 1807-1822 [PMID:15027873] |
| ChEMBL | Displacement of [3H]Ro 15-1788 from human recombinant GABAA alpha-1-beta-3-gamma-2 receptor expressed in L(tk-) cells | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2005) 48: 7089-7092 [PMID:16279764] |
| ChEMBL | Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-1-beta-3-gamma-2 | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| ChEMBL | Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-1-beta-3-gamma-2 subtype expressed in L (tk-) cells | B | 7.89 | pKi | 13 | nM | Ki | J Med Chem (2005) 48: 1367-1383 [PMID:15743180] |
| ChEMBL | Displacement of [3H]-Ro15-1788 from human recombinant GABAA alpha1 in combination with beta-3-gamma-2 expressed in L(tk-) cells | B | 7.89 | pKi | 13 | nM | Ki | J Med Chem (2006) 49: 35-38 [PMID:16392789] |
| ChEMBL | Displacement of [3H]Ro 15-1788 from recombinant human GABAA alpha-1 receptor plus beta3gamma2 expressed in L(tk-) cells | B | 7.89 | pKi | 13 | nM | Ki | J Med Chem (2006) 49: 1235-1238 [PMID:16480260] |
| 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 | 7.7 | pKi | 20 | nM | Ki | Bioorg Med Chem Lett (2022) 62: 128637-128637 [PMID:35218882] |
| GtoPdb | Assay using recombinant GABAA channels with subunit composition; α2β1γ2. | - | 7.77 | pKi | 16.9 | nM | Ki | Science (1989) 245: 1389-92 [PMID:2551039] |
| GABAA receptor γ2 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-2/beta-2/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111327] [GtoPdb: 414, 405, 411] [UniProtKB: P18508, P23576, P63138] | ||||||||
| ChEMBL | Binding affinity for recombinant rat GABA-A receptor alpha-2-beta-2-gamma-2 subunits expressed in HEK293 cells | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2003) 46: 310-313 [PMID:12519068] |
| 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 | Displacement of [3H] Ro15-1788 from recombinant human GABAA alpha2 receptor plus beta-3-gamma-2 expressed in L(tk-) cells | B | 7.48 | pKi | 33 | nM | Ki | J Med Chem (2006) 49: 1235-1238 [PMID:16480260] |
| ChEMBL | Binding affinity towards human gamma-aminobutyric-acid A receptor alpha-2-beta-3-gamma-2 using [3H]Ro-151788 expressed in L(tk-) cells | B | 7.58 | pKi | 26.2 | nM | Ki | J Med Chem (2004) 47: 3642-3657 [PMID:15214791] |
| ChEMBL | Binding affinity for human GABA-A receptor alpha-2-beta-3-gamma-2 subunits in L(tk-) cells | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2004) 47: 1807-1822 [PMID:15027873] |
| ChEMBL | Displacement of [3H]Ro 15-1788 from human recombinant GABAA alpha-2-beta-3-gamma-2 receptor expressed in L(tk-) cells | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2005) 48: 7089-7092 [PMID:16279764] |
| ChEMBL | Binding affinity to human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-2-beta-3-gamma-2 | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| GtoPdb | Assay using recombinant GABAA channels with subunit composition; α2β1γ2. | - | 7.77 | pKi | 16.9 | nM | Ki | Science (1989) 245: 1389-92 [PMID:2551039] |
| ChEMBL | Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric acid A receptor alpha-2-beta-3-gamma-2 subtype expressed in L (tk-) cells | B | 8.18 | pKi | 6.6 | nM | Ki | J Med Chem (2005) 48: 1367-1383 [PMID:15743180] |
| ChEMBL | Binding affinity evaluated by ability to displace [3H]-Ro-15-1788 from recombinant human Gamma-aminobutyric acid A receptor alpha-2-beta-3-gamma-2 expressed in L(tk-)cells | B | 8.18 | pKi | 6.6 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1381-1384 [PMID:10890169] |
| ChEMBL | Displacement of [3H]-Ro15-1788 from human recombinant GABAA alpha2 in combination with beta3gamma2 expressed in L(tk-) cells | B | 8.18 | pKi | 6.6 | nM | Ki | J Med Chem (2006) 49: 35-38 [PMID:16392789] |
| ChEMBL | Binding affinity to human alpha2beta3gamma2 GABA receptor expressed in Xenopus laevis oocytes | B | 7.46 | pEC50 | 35 | nM | EC50 | Bioorg Med Chem (2010) 18: 8374-8382 [PMID:20980155] |
| 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] | ||||||||
| GtoPdb | Assay using recombinant GABAA channels with subunit composition; α3β1γ2. | - | 7.77 | pKi | 17 | nM | Ki | Science (1989) 245: 1389-92 [PMID:2551039] |
| ChEMBL | Displacement of [3H]flunitrazepam from human recombinant alpha3beta2gamma2 GABAA receptor expressed in HEK cell membrane by competitive radioligand binding assay | B | 7.82 | pKi | 15 | nM | Ki | Bioorg Med Chem Lett (2022) 62: 128637-128637 [PMID:35218882] |
| ChEMBL | Displacement of [3H]Flumazenil from human GABA-Aalpha3 receptor plus beta-2-gamma-2 expressed in HEK293 cells | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2006) 49: 2526-2533 [PMID:16610795] |
| ChEMBL | Displacement of [3H]flunitrazepam from GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in Sf9 cells | B | 8 | pKi | 10 | nM | Ki | J Med Chem (1996) 39: 158-175 [PMID:8568803] |
| GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111343] [GtoPdb: 414, 406, 411] [UniProtKB: P18508, P20236, P63138] | ||||||||
| ChEMBL | Binding affinity for rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells | B | 7.77 | pKi | 17 | nM | Ki | J Med Chem (1994) 37: 4576-4580 [PMID:7799410] |
| ChEMBL | Binding affinity for recombinant rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2003) 46: 310-313 [PMID:12519068] |
| ChEMBL | Displacement of [3H]Ro15-1788 from rat recombinant GABA alpha-3-beta-2-gamma-2 receptor expressed in HEK293 cells | B | 7.85 | pKi | 14 | nM | Ki | Bioorg Med Chem (2007) 15: 2573-2586 [PMID:17306981] |
| ChEMBL | Displacement of [3H]Ro-151788 from rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells | B | 7.86 | pKi | 13.9 | nM | Ki | J Med Chem (2002) 45: 5710-5720 [PMID:12477354] |
| 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] | ||||||||
| ChEMBL | Binding affinity evaluated by ability to displace [3H]Ro-151788 from recombinant human Gamma-aminobutyric acid A receptor alpha-3-beta-3-gamma-2 expressed in L(tk-)cells | B | 7.48 | pKi | 33 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1381-1384 [PMID:10890169] |
| ChEMBL | Displacement of [3H]Ro-151788 from human recombinant GABAA alpha3 in combination with beta3gamma2 expressed in L(tk-) cells | B | 7.48 | pKi | 33 | nM | Ki | J Med Chem (2006) 49: 35-38 [PMID:16392789] |
| ChEMBL | Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-3-beta-3-gamma-2 subtype expressed in L (tk-) cells | B | 7.48 | pKi | 33 | nM | Ki | J Med Chem (2005) 48: 1367-1383 [PMID:15743180] |
| ChEMBL | Binding affinity towards human gamma-aminobutyric-acid A receptor alpha-3-beta-3-gamma-2 using [3H]Ro-151788 expressed in L(tk-) cells | B | 7.63 | pKi | 23.7 | nM | Ki | J Med Chem (2004) 47: 3642-3657 [PMID:15214791] |
| GtoPdb | Assay using recombinant GABAA channels with subunit composition; α3β1γ2. | - | 7.77 | pKi | 17 | nM | Ki | Science (1989) 245: 1389-92 [PMID:2551039] |
| ChEMBL | Binding affinity for human GABA-A receptor alpha-3-beta-3-gamma-2 subunits in L(tk-) cells | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2004) 47: 1807-1822 [PMID:15027873] |
| ChEMBL | Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-3-beta-3-gamma-2 | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| ChEMBL | Displacement of [3H]Ro 15-1788 from human recombinant GABAA alpha-3-beta-3-gamma-2 receptor expressed in L(tk-) cells | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2005) 48: 7089-7092 [PMID:16279764] |
| ChEMBL | Binding affinity to human alpha3beta3gamma2 GABA receptor expressed in Xenopus laevis oocytes | B | 6.88 | pEC50 | 131 | nM | EC50 | Bioorg Med Chem (2010) 18: 8374-8382 [PMID:20980155] |
| GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor β3 subunit/GABA A receptor alpha-5/beta-3/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111374] [GtoPdb: 414, 408, 412] [UniProtKB: P18508, P19969, P63079] | ||||||||
| ChEMBL | Binding affinity for recombinant rat GABA-A receptor alpha-5-beta-3-gamma-2 subunits expressed in HEK 293 cells | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (2003) 46: 310-313 [PMID:12519068] |
| ChEMBL | Displacement of [3H]flumazenil from rat GABA-A alpha-5-beta-3-gamma-2 receptor expressed in HEK293 cells | B | 8.01 | pKi | 9.8 | nM | Ki | J Med Chem (2009) 52: 3723-3734 [PMID:19469479] |
| 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] | ||||||||
| ChEMBL | Binding affinity towards human alpha-5-beta-3-gamma-2 GABA-A receptor using [3H]Ro-151788 expressed in L(tk-) cells | B | 7.95 | pKi | 11.2 | nM | Ki | J Med Chem (2004) 47: 3642-3657 [PMID:15214791] |
| ChEMBL | Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-5-beta-3-gamma-2 | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| ChEMBL | Binding affinity for human GABA-A receptor alpha-5-beta-3-gamma-2 subunits in L(tk-) cells | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (2004) 47: 1807-1822 [PMID:15027873] |
| ChEMBL | Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-5-beta-3-gamma-2 subtype expressed in L (tk-) cells | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (2005) 48: 1367-1383 [PMID:15743180] |
| ChEMBL | Displacement of [3H]Ro-151788 from human recombinant GABAA alpha5 in combination with beta3gamma2 expressed in L(tk-) cells | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (2006) 49: 35-38 [PMID:16392789] |
| ChEMBL | Binding affinity to human recombinant GABAA alpha5beta3gamma2 expressed in Xenopus laevis oocytes by patch clamp technique | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2013) 56: 593-624 [PMID:23121096] |
| ChEMBL | Binding affinity to human alpha5beta3gamma2 GABA receptor expressed in Xenopus laevis oocytes | B | 7.35 | pEC50 | 45 | nM | EC50 | Bioorg Med Chem (2010) 18: 8374-8382 [PMID:20980155] |
| GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABAA receptor α6 subunit/GABA A receptor alpha-6/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111370] [GtoPdb: 414, 411, 409] [UniProtKB: P18507, P47870, Q16445] | ||||||||
| ChEMBL | Displacement of [3H]-Ro-15-4513 from GABA-A receptor alpha-6-beta-2-gamma-2 subunits expressed in Sf9 cells | B | 5.15 | pKi | >7000 | nM | Ki | J Med Chem (1996) 39: 158-175 [PMID:8568803] |
| ChEMBL | Displacement of [3H]-Ro- 15-4513 from alpha-6-beta-2-gamma-2 GABA-A receptor subunits expressed in Sf9 cell membranes | B | 5.15 | pKi | >7000 | nM | Ki | J Med Chem (1994) 37: 758-768 [PMID:8145225] |
| GABAA receptor γ2 subunit/GABAA receptor α6 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-6/beta-2/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111365] [GtoPdb: 414, 409, 411] [UniProtKB: P18508, P30191, P63138] | ||||||||
| ChEMBL | Binding affinity for rat GABA-A receptor alpha-6-beta-2-gamma-2 subunits expressed in HEK293 cells | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1994) 37: 4576-4580 [PMID:7799410] |
| ChEMBL | Displacement of [3H]-Ro- 15-4513 from alpha-6 beta2 gamma2 subunits of Rat GABA-A receptor expressed in Sf-9 insect cell membranes | B | 5.15 | pKi | >7000 | nM | Ki | J Med Chem (1996) 39: 4654-4666 [PMID:8917654] |
| ChEMBL | Binding affinity for mutant rat GABA-A receptor alpha-6-(his)-beta-2-gamma-2 subunits expressed in HEK293 cells | B | 7.01 | pKi | 98 | nM | Ki | J Med Chem (1994) 37: 4576-4580 [PMID:7799410] |
| ChEMBL | Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr)beta2gamma2 subunits expressed in HEK293 cells | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (1994) 37: 4576-4580 [PMID:7799410] |
| ChEMBL | Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr,gly)beta2gamma2 subunits expressed in HEK293 cells | B | 8.05 | pKi | 9 | nM | Ki | J Med Chem (1994) 37: 4576-4580 [PMID:7799410] |
| ChEMBL | Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr,gly,val)beta2gamma2 subunits expressed in HEK293 cells | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (1994) 37: 4576-4580 [PMID:7799410] |
| 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 | 5.52 | pKi | >3000 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| GABAA receptor π subunit/GABAA receptor δ subunit/GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABAA receptor α4 subunit/GABAA receptor ε subunit/GABAA receptor α6 subunit/GABAA receptor γ1 subunit/GABAA receptor γ3 subunit/GABAA receptor θ subunit/GABA-A receptor; anion channel in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093872] [GtoPdb: 419, 416, 404, 410, 414, 412, 408, 406, 405, 411, 407, 417, 409, 413, 415, 418] [UniProtKB: O00591, O14764, P14867, P18505, P18507, P28472, P31644, P34903, P47869, P47870, P48169, P78334, Q16445, Q8N1C3, Q99928, Q9UN88] | ||||||||
| GtoPdb | Assay using recombinant GABAA channels with subunit composition; α2β1γ2. | - | 7.77 | pKi | 16.9 | nM | Ki | Science (1989) 245: 1389-92 [PMID:2551039] |
| GtoPdb | Assay using recombinant GABAA channels with subunit composition; α3β1γ2. | - | 7.77 | pKi | 17 | nM | Ki | Science (1989) 245: 1389-92 [PMID:2551039] |
| GtoPdb | Assay using recombinant GABAA channels with subunit composition; α1β1γ2. | - | 7.79 | pKi | 16.3 | nM | Ki | Science (1989) 245: 1389-92 [PMID:2551039] |
| ChEMBL | Binding affinity towards Benzodiazepine receptor from bovine brain membrane using [3H]Ro-151788 as radioligand | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2002) 45: 5710-5720 [PMID:12477354] |
| ChEMBL | Displacement of [3H]flumazenil from bovine benzodiazepine receptor GABA-A channel of brain membranes | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2005) 48: 2936-2943 [PMID:15828832] |
| ChEMBL | Displacement of [35S]TBPS from GABA-A receptor complex at low umolar concentration | B | 4.13 | pIC50 | 74000 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 1941-1946 |
| ChEMBL | Binding affinity to the benzodiazepine receptor assayed using 0.5 nM [3H]flunitrazapam as radioligand in guinea pig cerebellum | B | 7.85 | pIC50 | -7.85 | nM | Log IC50 | Bioorg Med Chem Lett (1995) 5: 2397-2402 |
| ChEMBL | Binding affinity to the benzodiazepine receptor assayed using 0.5 nM [3H]flunitrazapam as radioligand in guinea pig cerebellum | B | 7.85 | pIC50 | 14.1 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2397-2402 |
| ChEMBL | In vitro displacement of [3H]flunitrazepam from GABA-A central benzodiazepine receptor of guinea pig cerebellum | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2391-2396 |
| ChEMBL | Percent inhibition against central Benzodiazepine receptor at 1 uM | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2005) 48: 6887-6896 [PMID:16250647] |
| ChEMBL | In vitro displacement of [3H]-diazepam from GABA-A Benzodiazepine receptor | B | 8.09 | pIC50 | 8.1 | nM | IC50 | J Med Chem (1982) 25: 1050-1055 [PMID:6127410] |
| ChEMBL | Inhibition of GABA-A receptor (unknown origin) | B | 8.38 | pIC50 | 4.2 | nM | IC50 | Eur J Med Chem (2021) 226: 113867-113867 [PMID:34607244] |
| GABA-A receptor; anion channel in Bovine (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094107] [UniProtKB: P08219, P08220, P10063, P10064, P20237, P22300] | ||||||||
| ChEMBL | Displacement of [3H]Ro-151788 from GABA-A benzodiazepine receptor of bovine brain membranes | B | 8 | pKi | 10 | nM | Ki | J Med Chem (1999) 42: 2218-2226 [PMID:10377227] |
| ChEMBL | Inhibition of [3H]Ro-151788 binding to GABA-A central benzodiazepine receptor of bovine brain membranes | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2003) 46: 310-313 [PMID:12519068] |
| ChEMBL | In vitro inhibition of [3H]flunitrazepam binding to GABA-A benzodiazepine receptor of bovine cerebral cortical membranes at 10 uM | B | 8 | pKi | 10 | nM | Ki | J Med Chem (1992) 35: 2214-2220 [PMID:1319492] |
| ChEMBL | Displacement of [3H]flumazenil from GABA-A receptor in bovine brain membranes | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2006) 49: 2489-2495 [PMID:16610792] |
| ChEMBL | Inhibition of [3H]flunitrazepam binding to GABA-A central Benzodiazepine receptor of bovine brain membranes | B | 7.39 | pIC50 | 41 | nM | IC50 | J Med Chem (1985) 28: 506-509 [PMID:2984422] |
| ChEMBL | Inhibition of [3H]flunitrazepam binding to benzodiazepine receptor in bovine brain membrane | B | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (1988) 31: 1-3 [PMID:2826782] |
| ChEMBL | Affinity to displace [3H]flunitrazepam from Benzodiazepine receptor in bovine brain membrane | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (1990) 33: 2646-2651 [PMID:2167984] |
| GABAA receptor α6 subunit/GABAA receptor γ2 subunit/GABAA receptor δ subunit/GABAA receptor α2 subunit/GABAA receptor α3 subunit/GABAA receptor γ3 subunit/GABAA receptor β1 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABAA receptor π subunit/GABAA receptor α4 subunit/GABAA receptor θ subunit/GABAA receptor γ1 subunit/GABA-A receptor; anion channel in Mouse (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094133] [GtoPdb: 409, 414, 416, 405, 406, 415, 410, 404, 412, 408, 419, 407, 418, 413] [UniProtKB: A2AMW3, P16305, P22723, P22933, P26048, P26049, P27681, P50571, P62812, P63080, Q8BHJ7, Q8QZW7, Q9D6F4, Q9JLF1, Q9R0Y8] | ||||||||
| ChEMBL | Binding affinity for umolar GABA-A central benzodiazepine receptor | B | 4.07 | pKi | 85000 | nM | Ki | J Med Chem (1984) 27: 772-778 [PMID:6330354] |
| ChEMBL | Displacement of [3H]flunitrazepam from GABA-A central benzodiazepine receptor of mouse brain | B | 7.92 | pIC50 | 12 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 1941-1946 |
| 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 | Inhibition of [3H]diazepam binding to GABA-A central benzodiazepine receptor of rat brain homogenate | B | 6.49 | pKi | 323 | nM | Ki | J Med Chem (1988) 31: 1115-1123 [PMID:2836588] |
| ChEMBL | Inhibition of [3H]diazepam binding to GABA-A central benzodiazepine receptor of rat brain homogenate | B | 6.84 | pKi | 144 | nM | Ki | J Med Chem (1988) 31: 1115-1123 [PMID:2836588] |
| ChEMBL | Displacement of [3H]flunitrazepam from GABA-A Benzodiazepine receptor of rat brain membranes | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (1990) 33: 2640-2645 [PMID:1975276] |
| ChEMBL | Binding affinity to rat benzodiazepine receptor | B | 7.85 | pKi | 14 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3215-3218 [PMID:12372537] |
| ChEMBL | Displacement of [3H]flunitrazepam at GABA-A benzodiazepine receptor in rat brain cortical membranes | B | 7.98 | pKi | 10.5 | nM | Ki | J Med Chem (1996) 39: 2915-2921 [PMID:8709126] |
| ChEMBL | In vitro affinity against Benzodiazepine receptor binding to rat cortical membranes (using [3H]- flumazenil as radioligand). | B | 8.07 | pKi | 8.5 | nM | Ki | J Med Chem (1999) 42: 4343-4350 [PMID:10543878] |
| ChEMBL | Inhibition of [3H]flunitrazepam [3H]FNZ) binding to GABA-A Benzodiazepine receptor of synaptosomal membranes from rat brain | B | 8.15 | pKi | ~7 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 373-378 |
| ChEMBL | Binding affinity to Wistar rat benzodiazepine receptor | B | 8.17 | pKi | 6.8 | nM | Ki | J Med Chem (2006) 49: 1855-1866 [PMID:16539371] |
| ChEMBL | Binding affinity for Diazepam-Sensitive fraction of GABA-A benzodiazepine receptors | B | 8.18 | pKi | 6.6 | nM | Ki | J Med Chem (1993) 36: 1001-1006 [PMID:8386769] |
| ChEMBL | Displacement of [3H]- flunitrazepam from rat GABA-A benzodiazepine receptor | B | 8.22 | pKi | 6 | nM | Ki | J Med Chem (1994) 37: 758-768 [PMID:8145225] |
| ChEMBL | Displacement of [3H]-diazepam from GABA-A benzodiazepine receptor of rat cerebral cortex | B | 8.3 | pKi | 5.02 | nM | Ki | J Med Chem (1987) 30: 454-455 [PMID:3029371] |
| ChEMBL | Binding affinity against benzodiazepine (BZ) receptor by displacing [3H]diazepam in cerebral cortex of Wistar rats | B | 8.3 | pKi | 5.02 | nM | Ki | J Med Chem (1988) 31: 1738-1745 [PMID:2842502] |
| ChEMBL | Displacing potential to [3H]diazepam binding to benzodiazepine receptor in Wistar rat cerebral cortex | B | 8.3 | pKi | 5.02 | nM | Ki | J Med Chem (1989) 32: 1213-1217 [PMID:2542554] |
| ChEMBL | In vitro inhibition of [3H]diazepam binding to benzodiazepine receptor in rat cerebral cortical membrane | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (1982) 25: 1081-1091 [PMID:6127411] |
| ChEMBL | Displacement of [3H]diazepam from rat cerebral cortex benzodiazepine receptor | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (1996) 39: 2844-2851 [PMID:8709114] |
| ChEMBL | Binding affinity against benzodiazepine receptor (BzR) in rat cortical membranes determined by competition experiments with radiolabeled [3H]flunitrazepam (Fnz) | B | 8.31 | pKi | 4.9 | nM | Ki | J Med Chem (1996) 39: 3820-3836 [PMID:8809170] |
| ChEMBL | Inhibition of [3H]flunitrazepam binding to GABA-A receptor of rat cortical membranes | B | 8.31 | pKi | 4.9 | nM | Ki | J Med Chem (1996) 39: 158-175 [PMID:8568803] |
| ChEMBL | Displacement of [3H]flunitrazepam from GABA-A benzodiazepine receptor of rat cortical membranes | B | 8.31 | pKi | 4.9 | nM | Ki | J Med Chem (1999) 42: 1123-1144 [PMID:10197957] |
| ChEMBL | Displacement of [3H]flunitrazepam from GABA-A benzodiazepine receptor of rat cortical membranes | B | 8.31 | pKi | 4.9 | nM | Ki | J Med Chem (1996) 39: 4654-4666 [PMID:8917654] |
| ChEMBL | In vitro binding affinity against benzodiazepine receptor using [3H]diazepam as radioligand | B | 8.54 | pKi | 2.9 | nM | Ki | J Med Chem (1985) 28: 1314-1319 [PMID:2993620] |
| ChEMBL | Inhibition of [3H]diazepam binding to GABA-A central benzodiazepine receptor of rat brain homogenate | B | 8.54 | pKi | 2.9 | nM | Ki | J Med Chem (1988) 31: 1115-1123 [PMID:2836588] |
| ChEMBL | Inhibition of Diazepam-Insensitive fraction of GABA-A benzodiazepine receptors | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1993) 36: 1001-1006 [PMID:8386769] |
| ChEMBL | Ability to allosterically modulate the binding of [35S]TBPS to gamma-aminobutyric-acid A receptor in rat brain cortical P2 membranes. | B | 7.04 | pIC50 | 91 | nM | IC50 | J Med Chem (1997) 40: 61-72 [PMID:9016329] |
| ChEMBL | Inhibition of radiolabeled antagonist [3H]-Ro- 15-1788 binding to benzodiazepine receptor from rat cortical membranes | B | 7.11 | pIC50 | 77 | nM | IC50 | J Med Chem (1989) 32: 2282-2291 [PMID:2552115] |
| ChEMBL | Displacement of [3H]flunitrazepam from GABA-A benzodiazepine receptor in synaptic membranes of rat cerebral cortex | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1985) 28: 683-685 [PMID:2985787] |
| ChEMBL | Binding affinity against benzodiazepine site of gamma-aminobutyric-acid A receptor of rat cerebral cortex by using [3H]flunitrazepam in the absence of GABA. | B | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (1995) 38: 16-20 [PMID:7837226] |
| ChEMBL | Binding affinity against the BZD site of the Gamma-aminobutyric acid A receptor in rat cerebral cortex using radioligand ([3H]flunitrazepam) assay in the absence of Gamma-aminobutyric acid | B | 7.55 | pIC50 | 28 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 333-338 |
| ChEMBL | Agonistic activity against specific binding of radioligand [3H]Ro-151788 to GABA-A Benzodiazepine receptor in rat cortex | B | 7.69 | pIC50 | 20.6 | nM | IC50 | J Med Chem (1993) 36: 1669-1673 [PMID:8388472] |
| ChEMBL | Inhibition of [3H]-Ro- 15-1788 binding to GABA-A benzodiazepine receptor in rat brain membrane | B | 7.69 | pIC50 | 20.6 | nM | IC50 | J Med Chem (1995) 38: 950-957 [PMID:7699711] |
| ChEMBL | Displacement of [3H]flunitrazepam from GABA-A receptor of rat cerebellar tissue | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2579-2583 [PMID:11086734] |
| ChEMBL | Displacement of [3H]flunitrazepam from GABA-A receptor of rat forebrain tissue | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2579-2583 [PMID:11086734] |
| ChEMBL | Displacement of [3H]flunitrazepam from GABAA central benzodiazepine receptor in Wistar rat brain membrane without cerebellum measured after 60 mins by scintillation counting analysis | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem (2022) 64: 116758-116758 [PMID:35472555] |
| ChEMBL | Inhibition of [3H]flunitrazepam binding to GABA-A Benzodiazepine receptor of Wistar rat cerebral cortex | B | 7.81 | pIC50 | 15.4 | nM | IC50 | J Med Chem (1990) 33: 3110-3116 [PMID:1977911] |
| ChEMBL | Binding affinity against the BZD site of the Gamma-aminobutyric acid A receptor in rat cerebral cortex using radioligand ([3H]flunitrazepam) assay in the presence of Gamma-aminobutyric acid | B | 7.89 | pIC50 | 13 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 333-338 |
| ChEMBL | Binding affinity against benzodiazepine site of gamma-aminobutyric-acid A receptor of rat cerebral cortex by using [3H]flunitrazepam in the presence of GABA 1 mM. | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (1995) 38: 16-20 [PMID:7837226] |
| ChEMBL | In vitro binding affinity for GABA-A receptor in rat cortical or hippocampal membranes using [3H]flunitrazepam | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (1990) 33: 2772-2777 [PMID:2170646] |
| ChEMBL | Inhibition of [3H]flunitrazepam binding to GABA-A benzodiazepine receptor of rat cerebellum | B | 8.03 | pIC50 | 9.3 | nM | IC50 | J Med Chem (1989) 32: 2561-2573 [PMID:2573731] |
| ChEMBL | In vitro inhibitory concentration of compound against benzodiazepine receptor from rat cerebral cortex using [3H]- flunitrazepam was evaluated | B | 8.09 | pIC50 | 8.1 | nM | IC50 | J Med Chem (1994) 37: 745-757 [PMID:8145224] |
| ChEMBL | Inhibition of [3H]flunitrazepam binding to GABA-A benzodiazepine receptor of rat cortex | B | 8.14 | pIC50 | 7.3 | nM | IC50 | J Med Chem (1989) 32: 2561-2573 [PMID:2573731] |
| ChEMBL | Displacement of [3H]flunitrazepam from benzodiazepine receptor of rat cerebral cortex membranes | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (1991) 34: 2993-3006 [PMID:1681105] |
| ChEMBL | Inhibition of [3H]diazepam binding to GABA-A benzodiazepine receptor of rat brain | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (1988) 31: 2235-2246 [PMID:2848124] |
| ChEMBL | Displacement of [3H]diazepam from rat brain GABA-A benzodiazepine receptor | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (1987) 30: 1229-1239 [PMID:2885419] |
| ChEMBL | Effect on [3H]flunitrazepam binding to Benzodiazepine receptor | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1991) 34: 1754-1756 [PMID:1674542] |
| ChEMBL | Inhibition of specific binding of 1.5 nM [3H]diazepam to rat brain benzodiazepine receptors | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1990) 33: 196-202 [PMID:1967311] |
| ChEMBL | In vitro inhibition of binding to the benzodiazepine receptor in rat cerebral cortical membrane using [3H]diazepam as radioligand | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1988) 31: 1854-1861 [PMID:2842507] |
| ChEMBL | Inhibition of [3H]flunitrazepam binding to GABA-A benzodiazepine receptor of rat cerebral cortex | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1989) 32: 2561-2573 [PMID:2573731] |
| ChEMBL | Concentration that inhibits binding of 1.5 nM [3H]diazepam to rat brain benzodiazepine receptor | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1989) 32: 1020-1024 [PMID:2540330] |
| ChEMBL | In vitro inhibitory concentration of compound against benzodiazepine receptor from rat cerebral cortex using [3H]- flunitrazepam was evaluated | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1994) 37: 745-757 [PMID:8145224] |
| ChEMBL | Inhibitory concentration against specific binding of [3H]diazepam to Benzodiazepine receptor in rat brain | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1990) 33: 1910-1914 [PMID:2163452] |
| ChEMBL | In vitro for inhibition of [3H]diazepam towards Benzodiazepine receptor from rat | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1981) 24: 592-600 [PMID:6113284] |
| ChEMBL | Binding affinity against central benzodiazepine receptor(CBR). | B | 8.25 | pIC50 | 5.6 | nM | IC50 | J Med Chem (1996) 39: 4275-4284 [PMID:8863805] |
| ChEMBL | In vitro inhibition of [3H]diazepam binding to rat GABA-A benzodiazepine receptor | B | 8.27 | pIC50 | 5.4 | nM | IC50 | J Med Chem (1983) 26: 367-372 [PMID:6681844] |
| ChEMBL | Displacement of [3H]diazepam binding in rat brain membranes | B | 8.27 | pIC50 | 5.4 | nM | IC50 | J Med Chem (1983) 26: 1596-1601 [PMID:6138437] |
| ChEMBL | Binding affinity measured by [3H]diazepam binding assay in rat | B | 8.27 | pIC50 | 5.4 | nM | IC50 | J Med Chem (1983) 26: 1589-1596 [PMID:6138436] |
| ChEMBL | In vitro displacement of [3H]diazepam from GABA-A benzodiazepine receptor | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1983) 26: 100-103 [PMID:6131127] |
| ChEMBL | In vitro inhibition of binding to GABA-A central benzodiazepine-receptor of rat brain | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1982) 25: 337-339 [PMID:6121916] |
| ChEMBL | In vitro affinity for BZD site on GABA-A receptor from rat cerebral cortex using radioligand [3H]flunitrazepam | B | 8.31 | pIC50 | 4.9 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 2381-2386 [PMID:12161138] |
| ChEMBL | In vitro inhibitory against Gamma-aminobutyric acid A receptor from rat cerebral cortex using [3H]flunitrazepam as the radioligand | B | 8.31 | pIC50 | 4.9 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1547-1552 [PMID:10386933] |
| ChEMBL | Displacement of [3H]flunitrazepam from GABA-A Benzodiazepine receptors in rat forebrain | B | 8.36 | pIC50 | 4.4 | nM | IC50 | J Med Chem (1991) 34: 2899-2906 [PMID:1680197] |
| ChEMBL | Displacement of [3H]diazepam from GABA-A Benzodiazepine receptor of rat forebrain | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (1991) 34: 281-290 [PMID:1846920] |
| GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867] | ||||||||
| ChEMBL | Binding affinity to GABAA alpha-1-beta-2-gamma-2 receptor | B | 7.44 | pKd | 36 | nM | Kd | J Med Chem (2008) 51: 3788-3803 [PMID:18537233] |
| GtoPdb | Assay using recombinant GABAA channels with subunit composition; α1β1γ2. | - | 7.79 | pKi | 16.3 | nM | Ki | Science (1989) 245: 1389-92 [PMID:2551039] |
| ChEMBL | Binding affinity to GABA-A alpha1 (unknown origin) | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2020) 63: 3425-3446 [PMID:31738537] |
| GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL343] [GtoPdb: 404] [UniProtKB: P62813] | ||||||||
| ChEMBL | Displacement of [3H]RO15-1788 from recombinant rat GABAalpha1 receptor expressed in HEK293 cells after 1 hr | B | 7.85 | pKi | 14 | nM | Ki | Eur J Med Chem (2017) 126: 298-352 [PMID:27894044] |
| GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4956] [GtoPdb: 405] [UniProtKB: P47869] | ||||||||
| ChEMBL | Binding affinity to GABA-A alpha2 (unknown origin) | B | 7.77 | pKi | 17 | nM | Ki | J Med Chem (2020) 63: 3425-3446 [PMID:31738537] |
| GtoPdb | Assay using recombinant GABAA channels with subunit composition; α2β1γ2. | - | 7.77 | pKi | 16.9 | nM | Ki | Science (1989) 245: 1389-92 [PMID:2551039] |
| GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL341] [GtoPdb: 405] [UniProtKB: P23576] | ||||||||
| ChEMBL | Displacement of [3H]RO15-1788 from recombinant rat GABAalpha2 receptor expressed in HEK293 cells after 1 hr | B | 7.7 | pKi | 20 | nM | Ki | Eur J Med Chem (2017) 126: 298-352 [PMID:27894044] |
| ChEMBL | Displacement of [3H]flumazenil from rat GABA-A alpha-2-beta-2-gamma-2 receptor expressed in HEK293 cells | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2009) 52: 3723-3734 [PMID:19469479] |
| GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3026] [GtoPdb: 406] [UniProtKB: P34903] | ||||||||
| ChEMBL | Binding affinity to GABA-A alpha3 (unknown origin) | B | 7.77 | pKi | 17 | nM | Ki | J Med Chem (2020) 63: 3425-3446 [PMID:31738537] |
| GtoPdb | Assay using recombinant GABAA channels with subunit composition; α3β1γ2. | - | 7.77 | pKi | 17 | nM | Ki | Science (1989) 245: 1389-92 [PMID:2551039] |
| GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL328] [GtoPdb: 406] [UniProtKB: P20236] | ||||||||
| ChEMBL | Displacement of [3H]RO15-1788 from recombinant rat GABAalpha3 receptor expressed in HEK293 cells after 1 hr | B | 7.82 | pKi | 15 | nM | Ki | Eur J Med Chem (2017) 126: 298-352 [PMID:27894044] |
| 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 | 7.64 | pKd | 23 | nM | Kd | J Med Chem (2008) 51: 3788-3803 [PMID:18537233] |
| ChEMBL | Binding affinity to GABA-A alpha5 (unknown origin) | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2020) 63: 3425-3446 [PMID:31738537] |
| GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL300] [GtoPdb: 408] [UniProtKB: P19969] | ||||||||
| ChEMBL | Displacement of [3H]RO15-1788 from recombinant rat GABAalpha5 receptor expressed in HEK293 cells after 1 hr | B | 7.96 | pKi | 11 | nM | Ki | Eur J Med Chem (2017) 126: 298-352 [PMID:27894044] |
| GABAA receptor γ1 subunit/GABA receptor gamma-1 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL296] [GtoPdb: 413] [UniProtKB: P23574] | ||||||||
| ChEMBL | Anxiolytic activity by displacement of [3H]diazepam from GABA-A receptor in rat synaptosomal membranes | F | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1980) 23: 952-955 [PMID:6105221] |
| GABAA receptor γ2 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit in Human [GtoPdb: 414, 409, 404, 412] [UniProtKB: P18507, Q16445, P14867, P28472] | ||||||||
| GtoPdb | Assay using recombinant GABAA channels with subunit composition; α1β1γ2. | - | 7.79 | pKi | 16.3 | nM | Ki | Science (1989) 245: 1389-92 [PMID:2551039] |
| GABAA receptor γ2 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/Gamma-aminobutyric acid receptor subunit alpha-1/alpha-6/beta-3/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL5291947] [GtoPdb: 414, 409, 404, 412] [UniProtKB: P18508, P30191, P62813, P63079] | ||||||||
| ChEMBL | Positive allosteric modulation of rat recombinant GABAA alpha6beta3alpha1-gamma2beta3 receptor expressed in Xenopus laevis oocytes assessed as increase in GABA-induced current amplitude at -80 mV holding potential in presence of GABA EC1 to 1.5 by two-electrode voltage-clamp assay | B | 4.74 | pEC50 | 18000 | nM | EC50 | Bioorg Med Chem (2019) 27: 3167-3178 [PMID:31186146] |
| GABAA receptor γ2 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit in Human [GtoPdb: 414, 404, 412] [UniProtKB: P18507, P14867, P28472] | ||||||||
| GtoPdb | Assay using recombinant GABAA channels with subunit composition; α1β1γ2. | - | 7.79 | pKi | 16.3 | nM | Ki | Science (1989) 245: 1389-92 [PMID:2551039] |
| GABAA receptor γ2 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/Gamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4296062] [GtoPdb: 414, 404, 412] [UniProtKB: P18508, P62813, P63079] | ||||||||
| ChEMBL | Positive allosteric modulation of rat recombinant GABAA alpha1beta3alpha1-gamma2beta3 receptor expressed in Xenopus laevis oocytes assessed as increase in GABA-induced current amplitude at -80 mV holding potential in presence of GABA EC1 to 1.5 by two-electrode voltage-clamp assay | B | 4.01 | pEC50 | 98000 | nM | EC50 | Bioorg Med Chem (2019) 27: 3167-3178 [PMID:31186146] |
| 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 | 7.96 | pKi | 11 | nM | Ki | Bioorg Med Chem Lett (2022) 62: 128637-128637 [PMID:35218882] |
| GABAA receptor γ2 subunit/GABAA receptor α6 subunit/GABAA receptor β3 subunit/Gamma-aminobutyric acid receptor subunit alpha-6/beta-3/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4296054] [GtoPdb: 414, 409, 412] [UniProtKB: P18508, P30191, P63079] | ||||||||
| ChEMBL | Positive allosteric modulation of rat recombinant GABAA alpha6beta3alpha6-gamma2beta3 receptor expressed in Xenopus laevis oocytes assessed as increase in GABA-induced current amplitude at -80 mV holding potential in presence of GABA EC1 to 1.5 by two-electrode voltage-clamp assay | B | 6.15 | pEC50 | 700 | nM | EC50 | Bioorg Med Chem (2019) 27: 3167-3178 [PMID:31186146] |
| ChEMBL | Positive allosteric modulation of rat recombinant GABAA alpha6beta3gamma2 receptor expressed in Xenopus laevis oocytes assessed as increase in GABA-induced current amplitude at -80 mV holding potential in presence of GABA EC1 to 1.5 by two-electrode voltage-clamp assay | B | 6.4 | pEC50 | 400 | nM | EC50 | Bioorg Med Chem (2019) 27: 3167-3178 [PMID:31186146] |
| Peripheral-type benzodiazepine receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2419] [UniProtKB: P30535] | ||||||||
| ChEMBL | Binding affinity to bovine brain membrane BzR assessed as inhibition constant | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2021) 64: 3508-3545 [PMID:33764065] |
| Translocator protein/Peripheral-type benzodiazepine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4552] [GtoPdb: 2879] [UniProtKB: P16257] | ||||||||
| ChEMBL | Binding affinity constant for peripheral (mitochondrial) Benzodiazepine receptor | B | 6.67 | pKd | 213 | nM | Kd | J Med Chem (1995) 38: 4730-4738 [PMID:7473601] |
| ChEMBL | Displacement of [3H]PK11195 from PBR in rat kidney mitochondrial membrane | B | 6.24 | pKi | 574 | nM | Ki | Bioorg Med Chem (2008) 16: 6145-6155 [PMID:18472268] |
| ChEMBL | Displacement of [3H]PK11195 from TSPO receptor in Sprague-Dawley rat cerebral cortex membrane by radiometric competitive assay | B | 6.71 | pIC50 | 194 | nM | IC50 | Eur J Med Chem (2015) 103: 210-222 [PMID:26355532] |
| TRH1 receptor in Rat [GtoPdb: 363] [UniProtKB: Q01717] | ||||||||
| GtoPdb | - | - | 5.15 | pKi | 7100 | nM | Ki | Ann N Y Acad Sci (1989) 553: 197-204 [PMID:2566295] |
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]
