AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: dexniguldipine
Target: Voltage-gated L-type calcium channel (Ion channel)
Gene: Cacna1c|Cacna1d|Cacna1s
UniProt: P22002|P27732|Q02485 (CAC1C_RAT|CAC1D_RAT|CAC1S_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.22
Assay: Inhibition of [3H]-isradipine binding to L-type [Ca2+] channel of rat brain membranes
Drug: dexniguldipine
Target: Voltage-gated L-type calcium channel (Ion channel)
Gene: CACNA1D|CACNA1C
UniProt: Q01668|Q13936 (CAC1D_HUMAN|CAC1C_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Assay: Mechanism of Action
Drug: dexamfetamine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Drug: dexamfetamine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.24
Assay: Inhibition of [3H]5-HT uptake at human SERT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay
Drug: dexamfetamine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7
Action type: INHIBITOR
Drug: dexamfetamine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.18
Drug: dexamfetamine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Drug: dexamfetamine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.68
Action type: RELEASING AGENT
Drug: dexamfetamine
Target: Cocaine- and amphetamine-regulated transcript protein (Transcription factor)
Gene: CARTPT
UniProt: Q16568 (CART_HUMAN)
Organism: Homo sapiens
Drug: dexamfetamine
Target: Amine oxidase [flavin-containing] A (Enzyme)
Gene: MAOA
UniProt: P21397 (AOFA_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.84
Assay: Inhibition of human recombinant MAOA by spectrophotometrically
Drug: dexamfetamine
Target: Synaptic vesicular amine transporter (Transporter)
Gene: SLC18A2
UniProt: Q05940 (VMAT2_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL1893; SINGLE PROTEIN
Drug: dexamfetamine
Target: Trace amine-associated receptor 1 (GPCR)
Gene: TAAR1
UniProt: Q96RJ0 (TAAR1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.87
Drug: dexamfetamine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: Slc6a4
UniProt: P31652 (SC6A4_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 5.75
Assay: Activity at SERT in rat synaptosomes obtained from whole brain minus striatum and cerebellum assessed as release of [3H]5-HT by liquid scintillation counting method
Drug: dexamfetamine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: Slc6a3
UniProt: P23977 (SC6A3_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.31
Assay: Inhibition of dopamine transporter-mediated [3H]dopamine uptake in Wistar rat striatal synaptosomes by liquid scintillation spectrometry
Drug: dexamfetamine
Target: Amine oxidase [flavin-containing] A (Enzyme)
Gene: Maoa
UniProt: P21396 (AOFA_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.91
Assay: Inhibition of MAOA in rat brain mitochondrial suspension
Drug: dexamfetamine
Target: Trace amine-associated receptor 1 (GPCR)
Gene: TAAR1
UniProt: Q8HZ64 (TAAR1_MACMU)
Organism: Macaca mulatta
Activity: EC50 = 6
Assay: Activation of rhesus monkey TAAR1 expressed in RD-HGA16 cells co-expressing Gq protein assessed as cAMP accumulation by fluorescence plate reader
Drug: dexamfetamine
Target: Trace amine-associated receptor 1 (GPCR)
Gene: Taar1
UniProt: Q923Y9 (TAAR1_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 7.25
Assay: Activation of rat wild type TAAR1 expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay
Drug: dexamfetamine
Target: Trace amine-associated receptor 1 (GPCR)
Gene: Taar1
UniProt: Q923Y8 (TAAR1_MOUSE)
Organism: Mus musculus
Activity: EC50 = 8.7
Assay: Activation of mouse TAAR1 expressed in human HEK293 cells assessed as accumulation of cAMP after 15 mins
Drug: dexamfetamine
Target: Serotonin (5-HT) receptor (GPCR)
Gene: Htr2c|Htr2a|Htr1a|Htr1b|Htr1d|Htr1f|Htr2b|Htr6|Htr7|Htr5a|Htr5b|Htr3a|Htr4|Htr3b
UniProt: P08909|P14842|P19327|P28564|P28565|P30940|P30994|P31388|P32305|P35364|P35365|P35563|Q62758|Q9JJ16 (5HT2C_RAT|5HT2A_RAT|5HT1A_RAT|5HT1B_RAT|5HT1D_RAT|5HT1F_RAT|5HT2B_RAT|5HT6R_RAT|5HT7R_RAT|5HT5A_RAT|5HT5B_RAT|5HT3A_RAT|5HT4R_RAT|5HT3B_RAT)
Organism: Rattus norvegicus
Activity: Kd = 5.35
Assay: Affinity against 5-hydroxytryptamine receptors in rat fundus model
Drug: dextromethorphan
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: D2 = 6.458
Action type: AGONIST
Drug: dextromethorphan
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.842
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: dextromethorphan
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: Ks = 4.48
Drug: dextromethorphan
Target: Glutamate receptor ionotropic, NMDA 3A (Ion channel)
Gene: GRIN3A
UniProt: Q8TCU5 (NMD3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.699
Action type: ANTAGONIST
Drug: dextromethorphan
Target: Glutamate receptor ionotropic, NMDA 2C (Ion channel)
Gene: GRIN2C
UniProt: Q14957 (NMDE3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.33
Action type: BLOCKER
Assay: Measured <i>vs.</i> exogenously expressed zeta1/epsilon3 (<i>GRIN1/GRIN2C</i>) subunits, at pH 6.9
Drug: dextromethorphan
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.98
Assay: Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
Drug: dextromethorphan
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: Sigmar1
UniProt: Q9R0C9 (SGMR1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.29
Assay: Binding affinity was measured as selectivity for sigma-1 site over muscarinic (M1) receptor in rat
Drug: dextromethorphan
Target: Sigma non-opioid intracellular receptor 1 (Membrane other)
Gene: SIGMAR1
UniProt: Q60492 (SGMR1_CAVPO)
Organism: Cavia porcellus
Activity: IC50 = 7.82
Assay: Displacement of [3H]pentazocine from sigma1 receptor in guinea pig membrane in presence of phenytoin
Drug: dextromethorphan
Target: Glutamate NMDA receptor (Ion channel)
Gene: Grin1|Grin2a|Grin2b|Grin2c|Grin2d|Grin3b|Grin3a
UniProt: P35439|Q00959|Q00960|Q00961|Q62645|Q8VHN2|Q9R1M7 (NMDZ1_RAT|NMDE1_RAT|NMDE2_RAT|NMDE3_RAT|NMDE4_RAT|NMD3B_RAT|NMD3A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.65
Assay: Binding affinity was measured against phencyclidine (PCP) receptor in rat using [3H]TCP as radioligand
Drug: dextromethorphan
Target: Sodium channel alpha subunits; brain (Types I, II, III) (Ion channel)
Gene: Scn1a|Scn2a|Scn3a
UniProt: P04774|P04775|P08104 (SCN1A_RAT|SCN2A_RAT|SCN3A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.89
Assay: Inhibition of [3H]batrachotoxin binding to rat brain sodium channel
Drug: dextromethorphan
Target: Taste receptor type 2 member 46 (GPCR)
Gene: TAS2R46
UniProt: P59540 (T2R46_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.51
Assay: Agonist activity at human TAS2R46 stably expressed in HEK293T/Galpha16-gustducin 44 cells assessed as effect on calcium flux by measuring deltaF/F0 ratio by Fluo-4-AM dye based FLIPR assay
Drug: dextropropoxyphene
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Drug: dextropropoxyphene
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Drug: dextropropoxyphene
Target: Glutamate receptor ionotropic, NMDA 3A (Ion channel)
Gene: GRIN3A
UniProt: Q8TCU5 (NMD3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.301
Drug: dextrothyroxine
Target: Thyroid hormone receptor beta (Transcription factor)
Gene: Thrb
UniProt: P18113 (THB_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.46
Assay: In vitro inhibition of the bound [125I]L-T3 rat liver nuclear L-triiodothyronine receptor
Drug: dextrothyroxine
Target: Thyroid hormone receptor (Nuclear hormone receptor)
Gene: THRA|THRB
UniProt: P10827|P10828 (THA_HUMAN|THB_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action; CHEMBL2111462; PROTEIN COMPLEX
Drug: dextrothyroxine
Target: Glutamate NMDA receptor (Ion channel)
Gene: Grin1|Grin2a|Grin2b|Grin2c|Grin2d|Grin3b|Grin3a
UniProt: P35439|Q00959|Q00960|Q00961|Q62645|Q8VHN2|Q9R1M7 (NMDZ1_RAT|NMDE1_RAT|NMDE2_RAT|NMDE3_RAT|NMDE4_RAT|NMD3B_RAT|NMD3A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.48
Assay: Ability to displace [3H]L-689560 from NMDA receptor glycine site in rat brain membranes
Drug: dezocine
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.42
Action type: PARTIAL AGONIST
Assay: Agonist activity at human cloned mu opioid receptor by [35S]GTPgammaS binding assay
Drug: dezocine
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Drug: diacerein
Target: Caspase-3 (Enzyme)
Gene: CASP3
UniProt: P42574 (CASP3_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.1
Assay: PUBCHEM_BIOASSAY: Absorbance-based biochemical high throughput dose response assay for activators of procaspase-3. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID463141, AID463197, AID463210, AID488941, AID488954, AID493114, AID493115, AID504328, AID504330]
Drug: diacerein
Target: Caspase-7 (Enzyme)
Gene: CASP7
UniProt: P55210 (CASP7_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.83
Assay: PUBCHEM_BIOASSAY: Counterscreen for procaspase-3 activators: absorbance-based biochemical high throughput dose response assay for activators of procaspase-7. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID463141, AID463197, AID463210, AID488941, AID488954, AID493114, AID493115, AID504328, AID504330]
Drug: diacerein
Target: Female germline-specific tumor suppressor gld-1 (Unclassified)
Gene: gld-1
UniProt: Q17339 (GLD1_CAEEL)
Organism: Caenorhabditis elegans
Activity: IC50 = 5.14
Assay: Active
Drug: diacerein
Target: N-acylethanolamine-hydrolyzing acid amidase (Enzyme)
Gene: NAAA
UniProt: Q02083 (NAAA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.16
Assay: Time dependent inhibition of recombinant human NAAA expressed in HEK293 cells by liquid scintillation counting method
Drug: diazepam
Target: GABA A receptor alpha-5/beta-2/gamma-3 (Ion channel)
Gene: GABRA5|GABRB2|GABRG3
UniProt: P31644|P47870|Q99928 (GBRA5_HUMAN|GBRB2_HUMAN|GBRG3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.203
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: diazepam
Target: Gamma-aminobutyric acid receptor subunit alpha-5 (Ion channel)
Gene: GABRA5
UniProt: P31644 (GBRA5_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.64
Assay: Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptor
Drug: diazepam
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.42
Drug: diazepam
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.1
Action type: ALLOSTERIC MODULATOR
Drug: diazepam
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.92
Assay: Inhibitory concentration against human Adenosine A3 receptor expressed in HEK293 cells using 0.1 nM [3H]AB-MECA
Drug: diazepam
Target: Aldo-keto reductase family 1 member C1 (Enzyme)
Gene: AKR1C1
UniProt: Q04828 (AK1C1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.25
Assay: 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) (
Drug: diazepam
Target: Aldo-keto reductase family 1 member C2 (Enzyme)
Gene: AKR1C2
UniProt: P52895 (AK1C2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.62
Assay: 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) (
Drug: diazepam
Target: Aldo-keto reductase family 1 member C3 (Enzyme)
Gene: AKR1C3
UniProt: P42330 (AK1C3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.08
Assay: 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) (
Drug: diazepam
Target: Fatty acid-binding protein, liver (Unclassified)
Gene: Fabp1
UniProt: P02692 (FABPL_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.27
Assay: 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
Drug: diazepam
Target: Acetylcholinesterase (Enzyme)
Gene: ache
UniProt: O42275 (ACES_ELEEL)
Organism: Electrophorus electricus
Activity: Ki = 4.89
Assay: Inhibition of Electrophorus electricus (electric eel) acetylcholinesterase (AChE) assessed as inhibition of ATCh hydrolysis by Ellman method
Drug: diazepam
Target: Translocator protein (Membrane receptor)
Gene: Tspo
UniProt: P16257 (TSPO_RAT)
Organism: Rattus norvegicus
Activity: Kd = 6.67
Assay: Binding affinity constant for peripheral (mitochondrial) Benzodiazepine receptor
Drug: diazepam
Target: Thyrotropin-releasing hormone receptor (GPCR)
Gene: Trhr
UniProt: Q01717 (TRFR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.15
Action type: ANTAGONIST
Drug: diazepam
Target: Cholinesterase (Enzyme)
Gene: BCHE
UniProt: P81908 (CHLE_HORSE)
Organism: Equus caballus
Activity: Ki = 7.37
Assay: Inhibition of Equus caballus (horse) serum butyrylcholinesterase (BChE) assessed as inhibition of BTCh hydrolysis by Ellman method
Drug: diazepam
Target: Gamma-aminobutyric acid receptor subunit alpha-1 (Ion channel)
Gene: Gabra1
UniProt: P62813 (GBRA1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.96
Assay: Displacement of [3H]flumazenil from rat GABA-A alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells
Drug: diazepam
Target: Gamma-aminobutyric acid receptor subunit alpha-2 (Ion channel)
Gene: Gabra2
UniProt: P23576 (GBRA2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.82
Assay: Displacement of [3H]flumazenil from rat GABA-A alpha-2-beta-2-gamma-2 receptor expressed in HEK293 cells
Drug: diazepam
Target: Gamma-aminobutyric acid receptor subunit alpha-5 (Ion channel)
Gene: Gabra5
UniProt: P19969 (GBRA5_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.01
Assay: Displacement of [3H]flumazenil from rat GABA-A alpha-5-beta-3-gamma-2 receptor expressed in HEK293 cells
Drug: diazepam
Target: GABA-A receptor alpha-1/beta-2/gamma-2 (Ion channel)
Gene: GABRA1|GABRG2|GABRB2
UniProt: P14867|P18507|P47870 (GBRA1_HUMAN|GBRG2_HUMAN|GBRB2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.143
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: diazepam
Target: GABA-A receptor alpha-2/beta-3/gamma-2 (Ion channel)
Gene: GABRG2|GABRB3|GABRA2
UniProt: P18507|P28472|P47869 (GBRG2_HUMAN|GBRB3_HUMAN|GBRA2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.699
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: diazepam
Target: GABA-A receptor alpha-3/beta-3/gamma-2 (Ion channel)
Gene: GABRG2|GABRB3|GABRA3
UniProt: P18507|P28472|P34903 (GBRG2_HUMAN|GBRB3_HUMAN|GBRA3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.65
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: diazepam
Target: GABA-A receptor alpha-5/beta-3/gamma-2 (Ion channel)
Gene: GABRG2|GABRB3|GABRA5
UniProt: P18507|P28472|P31644 (GBRG2_HUMAN|GBRB3_HUMAN|GBRA5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.959
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: diazepam
Target: GABA-A receptor alpha-1/beta-2/gamma-3 (Ion channel)
Gene: GABRA1|GABRB2|GABRG3
UniProt: P14867|P47870|Q99928 (GBRA1_HUMAN|GBRB2_HUMAN|GBRG3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.705
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: diazepam
Target: GABA-A receptor alpha-1/beta-3/gamma-2 (Ion channel)
Gene: GABRA1|GABRG2|GABRB3
UniProt: P14867|P18507|P28472 (GBRA1_HUMAN|GBRG2_HUMAN|GBRB3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.854
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: diazepam
Target: GABA-A receptor; anion channel (Ion channel)
Gene: Gabrp|Gabrb1|Gabrd|Gabrg2|Gabra5|Gabra3|Gabrg1|Gabra2|Gabra4|Gabrg3|Gabra6|Gabra1|Gabrb3|Gabrb2|Gabrq|Gabre
UniProt: O09028|P15431|P18506|P18508|P19969|P20236|P23574|P23576|P28471|P28473|P30191|P62813|P63079|P63138|Q91ZM7|Q9ES14 (GBRP_RAT|GBRB1_RAT|GBRD_RAT|GBRG2_RAT|GBRA5_RAT|GBRA3_RAT|GBRG1_RAT|GBRA2_RAT|GBRA4_RAT|GBRG3_RAT|GBRA6_RAT|GBRA1_RAT|GBRB3_RAT|GBRB2_RAT|Q91ZM7_RAT|GBRE_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.54
Assay: In vitro binding affinity against benzodiazepine receptor using [3H]diazepam as radioligand
Drug: diazepam
Target: GABA-A receptor; anion channel (Ion channel)
Gene: GABRA1|GABRB1|GABRA2|GABRA3|GABRA4|GABRG2
UniProt: P08219|P08220|P10063|P10064|P20237|P22300 (GBRA1_BOVIN|GBRB1_BOVIN|GBRA2_BOVIN|GBRA3_BOVIN|GBRA4_BOVIN|GBRG2_BOVIN)
Organism: Bos taurus
Activity: Ki = 8
Assay: Displacement of [3H]Ro-151788 from GABA-A benzodiazepine receptor of bovine brain membranes
Drug: diazepam
Target: GABA A receptor alpha-3/beta-2/gamma-2 (Ion channel)
Gene: Gabrg2|Gabra3|Gabrb2
UniProt: P18508|P20236|P63138 (GBRG2_RAT|GBRA3_RAT|GBRB2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.86
Assay: Displacement of [3H]Ro-151788 from rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells
Drug: diazepam
Target: GABA A receptor alpha-6/beta-2/gamma-2 (Ion channel)
Gene: Gabrg2|Gabra6|Gabrb2
UniProt: P18508|P30191|P63138 (GBRG2_RAT|GBRA6_RAT|GBRB2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.68
Assay: Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr,gly,val)beta2gamma2 subunits expressed in HEK293 cells
Drug: diazepam
Target: GABA-A receptor; alpha-1/beta-2/gamma-2 (Ion channel)
Gene: Gabrg2|Gabra1|Gabrb2
UniProt: P18508|P62813|P63138 (GBRG2_RAT|GBRA1_RAT|GBRB2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.92
Assay: Displacement of [3H]Ro15-1788 from rat recombinant GABA alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells
Drug: diazepam
Target: GABA-A receptor; anion channel (Ion channel)
Gene: Gabre|Gabra6|Gabrg2|Gabrd|Gabra2|Gabra3|Gabrg3|Gabrb1|Gabra1|Gabrb3|Gabra5|Gabrp|Gabra4|Gabrq|Gabrg1
UniProt: A2AMW3|P16305|P22723|P22933|P26048|P26049|P27681|P50571|P62812|P63080|Q8BHJ7|Q8QZW7|Q9D6F4|Q9JLF1|Q9R0Y8 (A2AMW3_MOUSE|GBRA6_MOUSE|GBRG2_MOUSE|GBRD_MOUSE|GBRA2_MOUSE|GBRA3_MOUSE|GBRG3_MOUSE|GBRB1_MOUSE|GBRA1_MOUSE|GBRB3_MOUSE|GBRA5_MOUSE|GBRP_MOUSE|GBRA4_MOUSE|GBRT_MOUSE|GBRG1_MOUSE)
Organism: Mus musculus
Activity: Ki = 4.07
Assay: Binding affinity for umolar GABA-A central benzodiazepine receptor
Drug: diazepam
Target: GABA A receptor alpha-2/beta-2/gamma-2 (Ion channel)
Gene: Gabrg2|Gabra2|Gabrb2
UniProt: P18508|P23576|P63138 (GBRG2_RAT|GBRA2_RAT|GBRB2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.7
Assay: Binding affinity for recombinant rat GABA-A receptor alpha-2-beta-2-gamma-2 subunits expressed in HEK293 cells
Drug: diazepam
Target: GABA A receptor alpha-5/beta-3/gamma-2 (Ion channel)
Gene: Gabrg2|Gabra5|Gabrb3
UniProt: P18508|P19969|P63079 (GBRG2_RAT|GBRA5_RAT|GBRB3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.96
Assay: Binding affinity for recombinant rat GABA-A receptor alpha-5-beta-3-gamma-2 subunits expressed in HEK 293 cells
Drug: diazepam
Target: GABA A receptor alpha-3/beta-2/gamma-2 (Ion channel)
Gene: GABRG2|GABRA3|GABRB2
UniProt: P18507|P34903|P47870 (GBRG2_HUMAN|GBRA3_HUMAN|GBRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.939
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: diazepam
Target: GABA A receptor alpha-3/beta-2/gamma-3 (Ion channel)
Gene: GABRA3|GABRB2|GABRG3
UniProt: P34903|P47870|Q99928 (GBRA3_HUMAN|GBRB2_HUMAN|GBRG3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.665
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: diazepam
Target: GABA A receptor alpha-5/beta-3/gamma-3 (Ion channel)
Gene: GABRB3|GABRA5|GABRG3
UniProt: P28472|P31644|Q99928 (GBRB3_HUMAN|GBRA5_HUMAN|GBRG3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.203
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: diazepam
Target: GABA A receptor alpha-5/beta-2/gamma-2 (Ion channel)
Gene: GABRG2|GABRA5|GABRB2
UniProt: P18507|P31644|P47870 (GBRG2_HUMAN|GBRA5_HUMAN|GBRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.004
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: diazoxide
Target: Nicotinamide phosphoribosyltransferase (Enzyme)
Gene: NAMPT
UniProt: P43490 (NAMPT_HUMAN)
Organism: Homo sapiens
Activity: Kd = 3.64
Assay: Binding affinity to NAMPT (2 to 491) (unknown origin) by surface plasmon resonance analysis
Drug: diazoxide
Target: Sulfonylurea receptor 1, Kir6.2 (Ion channel)
Gene: ABCC8|KCNJ11
UniProt: Q09428|Q14654 (ABCC8_HUMAN|KCJ11_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.63
Action type: OPENER
Assay: Activation of human recombinant SUR1/Kir6.2 channel expressed in HEK293 cells assessed as increase in ionic current by whole cell patch clamp assay
Drug: diazoxide
Target: ATP-sensitive inward rectifier potassium channel 11 (Ion channel)
Gene: Kcnj11
UniProt: Q61743 (KCJ11_MOUSE)
Organism: Mus musculus
Activity: EC50 = 4.2
Action type: ACTIVATOR